| Identification | Back Directory | [Name]
N-Cyclopropyl-2,4-difluoro-5-[[[2-(2-pyridinylamino)-5-thiazolyl]methyl]amino]benzamide | [CAS]
639858-32-5 | [Synonyms]
BMS 605541
N-Cyclopropyl-2,4-difluoro-5-[[[2-(2-pyridinylamino)-5-thiazolyl]methyl]amino]benzamide | [Molecular Formula]
C19H17F2N5OS | [MDL Number]
MFCD31579860 | [MOL File]
639858-32-5.mol | [Molecular Weight]
401.43 |
| Chemical Properties | Back Directory | [density ]
1.44±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
13.70±0.20(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
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 |
| [IC 50]
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) | [storage]
Store at -20°C | [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. DOI:10.1021/jm060347y |
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BOC Sciences
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| Website: |
https://www.bocsci.com |
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