| Bioactivity | BMS-605541 is a selective and orally active inhibitor of VEGFR-2 kinase with an IC50 value of 23 nM and Ki value of 49 nM. BMS-605541 inhibits the activity of Flk-1, VEGFR-1 and PDGFR-β with IC50 values of 40 nM, 400 nM and 200 nM, respectively. BMS-605541 can be used for cancer research[1]. | ||||||||||||
| Invitro | BMS-605541 (Compound 14) 通过 VEGF 抑制 HUVECs 的生长,IC50 值为 25 nM[1]。 | ||||||||||||
| In Vivo | BMS-605541 (12.5-180 mg/kg;一天 1 次或一天 2 次,持续 14 天) 对皮下植入 L2987 和 HCT-116 异种移植物的无胸腺小鼠具有抗肿瘤活性[1]。BMS-605541 的药代动力学 (PK) 参数[1]Species | ||||||||||||
| Name | BMS-605541 | ||||||||||||
| CAS | 639858-32-5 | ||||||||||||
| Formula | C19H17F2N5OS | ||||||||||||
| Molar Mass | 401.43 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Borzilleri RM, et al. Discovery and evaluation of N-cyclopropyl- 2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5- ylmethyl)amino)benzamide (BMS-605541), a selective and orally efficacious inhibitor of vascular endothelial growth factor receptor-2. J Med Chem. 2006 Jun 29;49(13):3766-9. |