Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3, and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, respectively, in cell-free trials. 69 nM/37 nM/108 nM and 59 nM/65 nM. Phase 3.

 

Brand: BCM

 

Target: VEGFR; FGFR; FLT; PDGFR; Src

 

Signaling Pathways: Angiogenesis; Tyrosine Kinase/Adaptors

 

In Vitro: BIBF1120 has little inhibitory effect on tyrosine kinase receptors such as EGFR, HER2, InsR, IGF1R or cell cycle kinases CDK1, CDK2 and CDK4, with IC50 greater than 1x103nM. BIBF1120 strongly inhibits VEGF-stimulated HUVEC and VEGF-stimulated HSMEC with EC50 of 9 and 7 nM, respectively. In contrast, when BIBF1120 acts on FaDu, the EC50 is hundreds of times larger for Calu-6 and Hela.

 

Melting Point: >237oC (dec.)

 

Boiling Point: 742.2±60.0 °C(Predicted)

 

pKa: 11.06±0.20(Predicted)

 

Solubility: Soluble in DMSO. Insoluble in Water; insoluble in Ethanol.

 

Isomeric SMILES: CN1CCN(CC1)CC(=O)N(C)C2=CC=C(C=C2)N=C(C3=CC=CC=C3)C4=C(NC5=C4C=CC(=C5)C(=O)OC)O  

 

InChIKey: CPMDPSXJELVGJG-UHFFFAOYSA-N  

 

InChI: InChI=1S/C31H33N5O4/c1-34-15-17-36(18-16-34)20-27(37)35(2)24-12-10-23(11-13-24)32-29(21-7-5-4-6-8-21)28-25-14-9-22(31(39)40-3)19-26(25)33-30(28)38/h4-14,19,33,38H,15-18,20H2,1-3H3

 

Attribute
[CAS No.]	656247-17-5
[Formula]	C31H33N5O4
[Molecular]	539.64
[Chem Name]	methyl 2-hydroxy-3-[N-[4-[methyl-[2-(4-methylpiperazin-1-yl)acetyl]amino]phenyl]-C-phenylcarbonimidoyl]-1H-indole-6-carboxylate
[Synonym]	Nintedanib; Intedanib; BIBF 1120; VARGATEF; INTEDANIB;INTEDANIB BASE;BIBF 1120; VARGATEF; INTEDANIB;INTEDANIB BASE;尼达尼布;BIBF1120(尼达尼布);尼达尼布杂质(A-D);尼达尼布乙烷磺酸盐;尼达尼布杂质对照品
[EINECS]	1592732-453-0
[MDL No.]	MFCD11974012
[Form]	Yellow solid
[Storage]	Keep in dark place. Inert atmosphere, 2-8°C

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