BMS-605541

• CAT Number: I014268
• CAS Number: 639858-32-5
• Molecular Formula: C19H17F2N5OS
• Molecular Weight: 401.43
• Purity: ≥95%
• Synonyms: N-cyclopropyl-2,4-difluoro-5-[[2-(pyridin-2-ylamino)-1,3-thiazol-5-yl]methylamino]benzamide
• InChI: InChI=1S/C19H17F2N5OS/c20-14-8-15(21)16(7-13(14)18(27)25-11-4-5-11)23-9-12-10-24-19(28-12)26-17-3-1-2-6-22-17/h1-3,6-8,10-11,23H,4-5,9H2,(H,25,27)(H,22,24,26)
• InChIKey: CUPLTRAPYIXFAX-UHFFFAOYSA-N
• SMILES: C1CC1NC(=O)C2=CC(=C(C=C2F)F)NCC3=CN=C(S3)NC4=CC=CC=N4

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].
BMS-605541 (Compound 14) inhibits the growth of HUVECs through VEGF with an IC50 value of 25 nM[1].
BMS-605541 (12.5-180 mg/kg; once a day or twice a day for 14 days) has anti-tumor activity in thymic mice subcutaneously implanted with L2987 and HCT-116 xenografts[1].
Pharmacokinetic (PK) parameters of BMS-605541[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

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.
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