Category: 2927-71-1

The nomenclature of pyrimidines is straightforward. However, like other heterocyclics, tautomeric hydroxyl groups yield complications since they exist primarily in the cyclic amide form. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. For example, 2-hydroxypyrimidine is more properly named 2-pyrimidone. A partial list of trivial names of various pyrimidines exists. Computed Properties of 2927-71-1.

Eberl, H. Christian;Werner, Thilo;Reinhard, Friedrich B.;Lehmann, Stephanie;Thomson, Douglas;Chen, Peiling;Zhang, Cunyu;Rau, Christina;Muelbaier, Marcel;Drewes, Gerard;Drewry, David;Bantscheff, Marcus research published 《 Chemical proteomics reveals target selectivity of clinical Jak inhibitors in human primary cells》, the research content is summarized as follows. Kinobeads are a set of promiscuous kinase inhibitors immobilized on sepharose beads for the comprehensive enrichment of endogenously expressed protein kinases from cell lines and tissues. These beads enable chemoproteomics profiling of kinase inhibitors of interest in dose-dependent competition studies in combination with quant. mass spectrometry. We present improved bead matrixes that capture more than 350 protein kinases and 15 lipid kinases from human cell lysates, resp. A multiplexing strategy is suggested that enables determination of apparent dissociation constants in a single mass spectrometry experiment Miniaturization of the procedure enabled determining the target selectivity of the clin. BCR-ABL inhibitor dasatinib in peripheral blood mononuclear cell (PBMC) lysates from individual donors. Profiling of a set of Jak kinase inhibitors revealed kinase off-targets from nearly all kinase families underpinning the need to profile kinase inhibitors against the kinome. Potently bound off-targets of clin. inhibitors suggest polypharmacol., e.g. through MRCK alpha and beta, which bind to decernotinib with nanomolar affinity.

2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., Computed Properties of 2927-71-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is a nitrogenous base similar to benzene (a six-membered ring) and includes cytosine, thymine, and uracil as bases used for DNA or RNA. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. Pyrimidine also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Product Details of C4HCl2FN2.

Fan, Yan;Huang, Zhi;Wang, Xiaoshuang;Ma, Yakun;Li, Yongtao;Yang, Shengyong;Shi, Yi research published 《 Discovery of 12O-a novel oral multi-kinase inhibitor for the treatment of solid tumor》, the research content is summarized as follows. A novel series of pyrimidine-benzotriazole derivatives have been synthesized and evaluated for their anticancer activity against human solid tumor cell lines. The most promising mol. 12O was identified for its excellent antiproliferative activities, especially against the SiHa cell line with IC50 value as 0.009μM. Kinase inhibition assay assessed 12O was a potential multi-kinase inhibitor, which possessed potent inhibitory activities against cyclin-dependent kinases (CDKs) and fms-like tyrosine kinase (FLT) with IC50 values in the nanomolar range. Mol. docking studies illustrated that the introduction of triazole moiety in 12O was critical for CDKs inhibition. In addition, 12O inhibited cancer cell proliferation, colony-formation, and cell cycle progression and provoked apoptotic death in vitro. In an SiHa xenograft mouse model, a once-daily dose of compound 12O at 20 mg/kg significantly suppressed the tumor growth without obvious toxicity. Taken together, 12O provided valuable guide for further structural optimization for CDKs and FLT inhibitors.

Product Details of C4HCl2FN2, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogen atoms at positions 1 and 3 in the ring. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Product Details of C4HCl2FN2.

Deng, Zhou;Chen, Guyue;Liu, Shuang;Li, Yunzhan;Zhong, Jiaji;Zhang, Baoding;Li, Li;Huang, Huiying;Wang, Zheng;Xu, Qingyan;Deng, Xianming research published 《 Discovery of methyl 3-((2-((1-(dimethylglycyl)-5-methoxyindolin-6-yl)amino)-5-(trifluoro-methyl) pyrimidin-4-yl)amino)thiophene-2-carboxylate as a potent and selective polo-like kinase 1 (PLK1) inhibitor for combating hepatocellular carcinoma》, the research content is summarized as follows. Hepatocellular carcinoma (HCC) is the second leading cause of cancer-related death worldwide and targeted therapeutics exhibit limited success. Polo-like kinase 1 (PLK1), a Ser/Thr kinase, plays a pivotal role in cell-cycle regulation and is considered a promising target in HCC. Here, via structural optimization using both biochem. kinase assays and cellular antiproliferation assays, we discovered a potent and selective PLK1 kinase inhibitor, compound 31. Compound 31 exhibited biochem. activity with IC₅₀ of < 0.508 nM against PLK1 and a KINOMEscan selectivity score (S(1)) of 0.02 at a concentration of 1μM. Furthermore, 31 showed broad antiproliferative activity against a variety of cancer cell lines, with the lowest antiproliferative IC₅₀ (11.1 nM) in the HCC cell line HepG2. A detailed mechanistic study of 31 revealed that inhibition of PLK1 by 31 induces mitotic arrest at the G2/M phase checkpoint, thus leading to cancer cell apoptosis. Moreover, 31 exhibited profound antitumor efficacy in a xenograft mouse model. Collectively, these results establish compound 31 as a good starting point for the development of PLK1 targeted therapeutics for HCC.

Product Details of C4HCl2FN2, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. It is also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Quality Control of 2927-71-1.

Diao, Peng-Cheng;Lin, Wei-Yuan;Jian, Xie-Er;Li, Yan-Hong;You, Wen-Wei;Zhao, Pei-Liang research published 《 Discovery of novel pyrimidine-based benzothiazole derivatives as potent cyclin-dependent kinase 2 inhibitors with anticancer activity》, the research content is summarized as follows. To develop novel CDK2 inhibitors as anticancer agents, a series of novel pyrimidine-based benzothiazole derivatives I (R = 4-(S(O)₂NH₂), 4-(piperidin-1-yl), 3-F, etc.) and II (R¹ = H, F, Cl, Me, MeO; R² = H, Me, F; R³ = Me, NH₂) was designed and synthesized. Initial biol. evaluation demonstrated that some of target compounds displayed potent antitumor activity in vitro against five cancer cell lines. Especially, the analog II (R¹ = F; R² = H; R³ = NH₂) exhibited approx. potency with AZD5438 toward four cells including HeLa, HCT116, PC-3, and MDA-MB-231 with IC₅₀ values of 0.45, 0.70, 0.92, 1.80 μM, resp. More interestingly, the most highly active compound II (R¹ = F; R² = H; R³ = NH₂) in this study also possessed promising CDK2/cyclin A2 inhibitory activities with IC₅₀ values of 15.4 nM, which was almost 3-fold potent than pos. control AZD5438, and mol. docking studies revealed that the analog bound efficiently with the CDK2 binding site. Further studies indicated that compound II (R¹ = F; R² = H; R³ = NH₂) could induce cell cycle arrest and apoptosis in a concentration-dependent manner. These observations suggest that pyrimidine-benzothiazole hybrids represent a new class of CDK2 inhibitors and well worth further investigation aiming to generate potential anticancer agents.

Quality Control of 2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The systematic study of pyrimidines began in 1884 with Pinner, who synthesized derivatives by condensing ethyl acetoacetate with amidines. Pinner first proposed the name “pyrimidin” in 1885. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. The parent compound was first prepared by Gabriel and Colman in 1900, by conversion of barbituric acid to 2,4,6-trichloropyrimidine followed by reduction using zinc dust in hot water. Related Products of 2927-71-1.

Dittus, Lars;Werner, Thilo;Muelbaier, Marcel;Bantscheff, Marcus research published 《 Differential Kinobeads Profiling for Target Identification of Irreversible Kinase Inhibitors》, the research content is summarized as follows. Chemoproteomics profiling of kinase inhibitors with kinobeads enables the assessment of inhibitor potency and selectivity for endogenously expressed protein kinases in cell lines and tissues. Using a small panel of targeted covalent inhibitors, we demonstrate the importance of measuring covalent target binding in live cells. We present a differential kinobeads profiling strategy for covalent kinase inhibitors where a compound is added either to live cells or to a cell extract that enables the comprehensive assessment of inhibitor selectivity for covalent and noncovalent targets. We found that Acalabrutinib, CC-292, and Ibrutinib potently and covalently bind TEC family kinases, but only Ibrutinib also potently binds to BLK. ZAK was identified as a submicromolar affinity Ibrutinib off-target due to covalent modification of Cys22. In contrast to Ibrutinib, 5Z-7-Oxozeaenol reacted with Cys150 next to the DFG loop, demonstrating an alternative route to covalent inactivation of this kinase, e.g., to inhibit canonical TGF-β dependent processes.

Related Products of 2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The nomenclature of pyrimidines is straightforward. However, like other heterocyclics, tautomeric hydroxyl groups yield complications since they exist primarily in the cyclic amide form. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. For example, 2-hydroxypyrimidine is more properly named 2-pyrimidone. A partial list of trivial names of various pyrimidines exists. SDS of cas: 2927-71-1.

Chen, Xiaojing;Liu, Lu;Liu, Peng;Chen, Yingying;Lin, Dan;Yan, Hao;Yan, Qi;Wang, Yi;Qiu, Yinda;Fang, Bo;Huang, Huijing;Qian, Jianchang;Zhao, Yunjie;Du, Zhou;Zhang, Qianwen;Li, Xiaokun;Zheng, Xiaohui;Liu, Zhiguo research published 《 Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma》, the research content is summarized as follows. Herein design, synthesis and structure-activity relationships of novel pyrimidine-2,4-diamine derivatives I [R¹ = H, CF₃, Me; R² = F, Cl, Me, etc.; R¹R² = CH=CH-S], I [R⁴ = H, 2-OMe, 3-OMe, etc.; R⁵ = (indol-5-yl), (indol-4-yl), (1-methyl-1H-indol-5-yl), etc.], III [R⁴ = H, 2-OMe, 3-OMe, etc.; R⁵ = indazol-6-yl, (4-ethylpiperazin-1-yl), (indazol-6-yl), etc.] that selectively inhibit PDGFRα/β kinases was studied. The screening cascades revealed that I [R⁴ = 3-OMe; R⁵ = (4-Ethylpiperazin-1-yl)] was the preferred compound among these derivatives, with IC₅₀ values of 2.4 and 0.9 nM for PDGFRα and PDGFRβ, resp. Moreover, the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) experiment revealed that I [R⁴ = 3-OMe; R⁵ = (4-ethylpiperazin-1-yl)] has a substantial cytotoxic effect against all osteosarcoma cancer cell lines; I [R⁴ = 3-OMe; R⁵ = (4-Ethylpiperazin-1-yl)] also displayed robust antitumor effects and low toxicity in a xenograft model. Addnl., I [R⁴ = 3-OMe; R⁵ = (4-ethylpiperazin-1-yl)] showed excellent bioavailability (F = 62.9%), suitable half-life (T1/2 = 2.12 h), satisfactory metabolic stability, and weak CYP isoform inhibitory activity, suggesting that I [R⁴ = 3-OMe; R⁵ = (4-ethylpiperazin-1-yl)] was a potential drug candidate for PDGFR-driven osteosarcoma.

2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., SDS of cas: 2927-71-1

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The nomenclature of pyrimidines is straightforward. However, like other heterocyclics, tautomeric hydroxyl groups yield complications since they exist primarily in the cyclic amide form. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. For example, 2-hydroxypyrimidine is more properly named 2-pyrimidone. A partial list of trivial names of various pyrimidines exists. Application In Synthesis of 2927-71-1.

Chen, Xing;Yan, Yaoyao;Zhang, Zhaoyan;Zhang, Faming;Liu, Mingming;Du, Leran;Zhang, Haixia;Shen, Xiaobao;Zhao, Dahai;Shi, Jing Bo;Liu, Xinhua research published 《 Discovery and In Vivo Anti-inflammatory Activity Evaluation of a Novel Non-peptidyl Non-covalent Cathepsin C Inhibitor》, the research content is summarized as follows. Cathepsin C (Cat C) participates in inflammation and immune regulation by affecting the activation of neutrophil serine proteases (NSPs). Therefore, cathepsin C is an attractive target for treatment of NSP-related inflammatory diseases. Here, the complete discovery process of the first potent “non-peptidyl non-covalent cathepsin C inhibitor” was described with hit finding, structure optimization, and lead discovery. Starting with hit 14, structure-based optimization and structure-activity relationship study were comprehensively carried out, and lead compound 54 was discovered as a potent drug-like cathepsin C inhibitor both in vivo and in vitro. Also, compound 54 (with cathepsin C Enz IC₅₀ = 57.4 nM) exhibited effective anti-inflammatory activity in an animal model of chronic obstructive pulmonary disease. These results confirmed that the non-peptidyl and non-covalent derivative could be used as an effective cathepsin C inhibitor and encouraged us to continue further drug discovery on the basis of this finding.

Application In Synthesis of 2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. In nucleic acids, three types of nucleobases are pyrimidine derivatives: cytosine (C), thymine (T), and uracil (U). Formula: C4HCl2FN2.

Choi, Jang-Sik;Hwang, Hae-jun;Kim, Se-Won;Lee, Byung Il;Lee, Jaekyoo;Song, Ho-Juhn;Koh, Jong Sung;Kim, Jung-Ho;Lee, Phil Ho research published 《 Highly potent and selective pyrazolylpyrimidines as Syk kinase inhibitors》, the research content is summarized as follows. A series of pyrazolylpyrimidine scaffold based Syk inhibitors, e.g. I, were synthesized and evaluated for their biol. activities and selectivity. Lead optimization efforts provided compounds with potent Syk inhibition in both enzymic and TNF-α release assay.

Formula: C4HCl2FN2, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. It is also found in many synthetic compounds such as barbiturates and the HIV drug, zidovudine. Product Details of C4HCl2FN2.

Crew, Andrew P.;Raina, Kanak;Dong, Hanqing;Qian, Yimin;Wang, Jing;Vigil, Dominico;Serebrenik, Yevgeniy V.;Hamman, Brian D.;Morgan, Alicia;Ferraro, Caterina;Siu, Kam;Neklesa, Taavi K.;Winkler, James D.;Coleman, Kevin G.;Crews, Craig M. research published 《 Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1》, the research content is summarized as follows. Proteolysis Targeting Chimeras (PROTACs) are bifunctional mols. that recruit an E3 ligase to a target protein to facilitate ubiquitination and subsequent degradation of that protein. While the field of targeted degraders is still relatively young, the potential for this modality to become a differentiated and therapeutic reality is strong, such that both academic and pharmaceutical institutions are now entering this interesting area of research. In this paper, the authors describe a broadly applicable process for identifying degrader hits based around the serine/threonine kinase TANK-binding kinase 1 (TBK1), and have generalized the key structural elements associated with degradation activities. Compound I is a potent hit (TBK1 DC₅₀ = 12 nM, D_max = 96%) with excellent selectivity against a related kinase IKKε, which was further used as a chem. tool to assess TBK1 as a target in mutant K-Ras cancer cells.

Product Details of C4HCl2FN2, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., 2927-71-1.

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Pyrimidine is an aromatic heterocyclic organic compound similar to pyridine. One of the three diazines (six-membered heterocyclics with two nitrogen atoms in the ring), it has the nitrogen atoms at positions 1 and 3 in the ring. 2927-71-1, formula is C4HCl2FN2, Name is 2,4-Dichloro-5-fluoropyrimidine. The pyrimidine ring system has wide occurrence in nature as substituted and ring fused compounds and derivatives, including the nucleotides cytosine, thymine and uracil, thiamine (vitamin B1) and alloxan. Product Details of C4HCl2FN2.

Cao, Hengyi;Zhu, Guangya;Sun, Lin;Chen, Ge;Ma, Xinxin;Luo, Xiao;Zhu, Jidong research published 《 Discovery of new small molecule inhibitors targeting isocitrate dehydrogenase 1 (IDH1) with blood-brain barrier penetration》, the research content is summarized as follows. Isocitrate dehydrogenase 1 (IDH1), which catalyzes the conversion of isocitrate to α-ketoglutarate, is one of key enzymes in the tricarboxylic acid cycle (TCA). Hotspot mutation at Arg¹³² in IDH1 that alters the function of IDH1 by further converting the α-ketoglutarate(α-KG) to 2-hydroxyglutarate (2-HG) have been identified in a variety of cancers. Because the IDH1 mutations occur in a significant portion of gliomas and glioblastomas, it is important that IDH1 inhibitors have to be brain penetrant to treat IDH1-mutant brain tumors. Here we report the efforts to design and synthesize a novel serial of mutant IDH1 inhibitors with improved activity and the blood-brain barrier (BBB) penetration. We show that compound 5, (R)-4-((S)-1-fluoroethyl)-3-(2-(((S)-1-(7-(trifluoromethyl)4,5-dihydroimidazo[1,5-a]quinolin-3-yl)ethyl)amino)pyrimidin-4-yl)oxazolidin-2-one [2379528-08-0], exhibits good brain exposure and potent 2-HG inhibition in a HT1080-derived mouse xenograft model, which makes it a potential preclin. candidate to treat IDH1-mutant brain tumors.

2927-71-1, 2,4-Dichloro-5-fluoropyrimidine is a useful research compound. Its molecular formula is C4HCl2FN2 and its molecular weight is 166.97 g/mol. The purity is usually 95%.
2,4-Dichloro-5-fluoropyrimidine is an aromatic hydrocarbon that has been shown to inhibit the growth of mouse tumor cells in vitro. It also inhibits the production of amines by reacting with industrial chemicals and sodium carbonate. This compound has potent inhibitory activity against autoimmune diseases and cytotoxic potency on mcf-7 cells. Furthermore, 2,4-Dichloro-5-fluoropyrimidine has been shown to have a chlorinating effect on cancer cells., Product Details of C4HCl2FN2

Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia