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BMS 605541

Names

[ CAS No. ]:
639858-32-5

[ Name ]:
BMS 605541

[Synonym ]:
N-Cyclopropyl-2,4-difluoro-5-({[2-(2-pyridinylamino)-1,3-thiazol-5-yl]methyl}amino)benzamide
N-cyclopropyl-2,4-difluoro-5-((2-(pyridin-2-ylamino)thiazol-5-ylmethyl)amino)benzamide
N-cyclopropyl-2,4-difluoro-5-({[2-(pyridin-2-ylamino)-1,3-thiazol-5-yl]methyl}amino)benzamide
Benzamide, N-cyclopropyl-2,4-difluoro-5-[[[2-(2-pyridinylamino)-5-thiazolyl]methyl]amino]-

Biological Activity

[Description]:

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].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

[Target]

VEGFR-2:23 nM (IC50)

VEGFR-2:49 nM (Ki)

Flk-1:40 nM (IC50)

VEGFR-1:400 nM (IC50)

PDGFR-β:200 nM (IC50)


[In Vitro]

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 Administration manner Dose (mg/kg) Cmax (µM) Tmax (h) AUC (µM•h) T1/2 (h) MRT (h) Cl (mL/min•kg) Vss (L/kg) Fpo (%) Mouse Oral gavage 90 148 0.5 649 (0-24 h) 1.7 3.4 100 Mouse Intravenous injection 10 11.8 1.7 100 Rat Oral gavage 50 44.0 2.0 202 2.2 3.5 100 Rat Intravenous injection 10 13.6 1.1 100 Cyno Oral gavage 5 8.0 0.75 28.5 7.1 7.9 52 Cyno Intravenous injection 1 3.9 1.6 52

[References]

[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.  

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Molecular Formula ]:
C19H17F2N5OS

[ Molecular Weight ]:
401.433

[ Exact Mass ]:
401.112183

[ LogP ]:
1.95

[ Index of Refraction ]:
1.660

Related Compounds