A VEGFR

BIBF 1120 (esylate) – 500 mg

Brand:
Cayman
CAS:
656247-18-6
Storage:
-20
UN-No:
Non-Hazardous - /

BIBF 1120 is an inhibitor of the receptor tyrosine kinases VEGFR, FGFR, and PDGFR (IC50s = 13-34, 37-610, 59, and 65 nM for VEGFR1-3, FGFR1-4, PDGFRα, and PDGFRβ, respectively).{20204} It is selective for VEGFR, FGFR, and PDGFR over a panel of 33 kinases but does inhibit FLT3, LCK, LYN, and Src (IC50s = 16-156 nM). BIBF 1120 inhibits growth factor-dependent proliferation of human umbilical vascular endothelial cells (HUVECs), human microvascular skin endothelial cells (HSMECs), human umbilical artery smooth muscle cells (HUASMCs), and bovine retinal pericytes (BRPs; EC50s = 7-290 nM). In vivo, BIBF 1120 (100 mg/kg) reduces tumor microvessel density and the number of PDGFRβ-expressing perivascular cells in a FaDu head and neck small cell carcinoma mouse xenograft model. It also inhibits tumor growth in a Caki-1 renal cancer mouse xenograft model. Formulations containing BIBF 1120 have been used in the treatment of idiopathic pulmonary fibrosis and non-small cell lung cancer (NSCLC).  

 

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SKU: 31082 - 500 mg Category:

Description

A VEGFR, FGFR, and PDGFR inhibitor (IC50s = 13-34, 37-610, 59, and 65 nM for VEGFR1-3, FGFR1-4, PDGFRα, and PDGFRβ, respectively); selective for VEGFR, FGFR, and PDGFR over a panel of 33 kinases but does inhibit FLT3, LCK, LYN, and Src (IC50s = 16-156 nM); inhibits growth factor-dependent proliferation of HUVECs, HSMECs, HUASMCs, and BRPs (EC50s = 7-290 nM); reduces tumor microvessel density and the number of PDGFRβ-expressing perivascular cells in a FaDu head and neck small cell carcinoma mouse xenograft model at 100 mg/kg; inhibits tumor growth in a Caki-1 renal cancer mouse xenograft model

Formal name: (3Z)-2,3-dihydro-3-[[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl]amino]phenylmethylene]-2-oxo-1H-indole-6-carboxylic acid, methyl ester, monoethanesulfonate

Synonyms:  Nintedanib

Molecular weight: 649.8

CAS: 656247-18-6

Purity: ≥98%

Formulation: A solid

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