BMS-536924
Cat. No.：YN440073
CAS No. ：468740-43-4
规格
价格(RMB)
库存
| 产品名称: | BMS-536924 |
| CAS No.: | 468740-43-4 |
| Chemical Name: | 4-[[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-3-[7-methyl-5-(4-morpholinyl)-1H-benzimidazol-2-yl]-2(1H)-pyridinone |
| Synonyms: | HY-10262, CS-0117 |
| 分子量: | 479.96 |
| 分子式: | C₂₅H₂₆ClN₅O₃ |
| SMILES: | O=C1C(C2=NC3=CC(N4CCOCC4)=CC(C)=C3N2)=C(C=CN1)NC[C@@H](O)C5=CC=CC(Cl)=C5 |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | BMS-536924 是一种具有口服活性，竞争性和选择性的胰岛素样生长因子受体 (IGF-1R) 激酶和胰岛素受体 (IR) 抑制剂，IC50分别为 100 nM 和 73 nM。BMS-536924 具有抗癌活性。 |
| IC50和靶点: | |
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| Solvent & Solubility: |
Wittman, M., Carboni, J., Attar, R., et al.Discovery of a (1H-benzoimidazol-2-yl)-1H-pyridin-2-one (BMS-536924) inhibitor of insulin-like growth factor I receptor kinase with in vivo antitumor activityJ. Med. Chem.48(18),5639-5643(2005)
Kim, H.J., Litzenburger, B.C., Cui, X., et al.Constitutively active type I insulin-like growth factor receptor causes transformation and xenograft growth of immortalized mammary epithelial cells and is acompanied by an epithelial-to-mesenchymal transition mediated by NF-κB and snailMol. Cell. Biol.27(8),3165-3175(2007)
Litzenburger, B.C., Kim, H.J., Kuiatse, I., et al.BMS-536924 reverses IGF-IR-induced transformation of mammary epithelial cells and causes growth inhibition and polarization of MCF7 cellsClin. Cancer Res.15(1),226-237(2009)
Li, L., Sinz, M.W., Zimmermann, K., et al.An insulin-like growth factor 1 receptor inhibitor induces CYP3A4 expression through a pregnane X receptor-independent, noncanonical constitutive androstane receptor-related mechanismJ. Pharmacol. Exp. Ther.340(3),688-697(2012)
