Flumatinib (HH-GV-678) is a novel Bcr-Abl inhibitor with IC50 values of 1.2 nM, 307.6 nM and 665.5 nM for c-Abl, PDGFRβ and c-Kit, respectively.

 

Brand: BCM

 

Target: Bcr-Abl; PDGFR; c-Kit

 

Signaling Pathways: Angiogenesis; Cytoskeletal Signaling; Tyrosine Kinase/Adaptors

 

In Vitro: In higher concentration, HH-GV-678 can inhibit the phosphorylation of c-Kit in Mo7e cell and the phosphorylation of PDGFR in Swiss3T3 cell, however, HH-GV-678 has no or little effect on other tyrosine kinases including EGFR, KDR, c-Src and HER2. HH-GV-678 can predominantly inhibit the autophosphorylation of Bcr-Abl in K562 cell. Flumatinib effectively overcame the drug resistance of certain KIT mutants with activation loop mutations (i.e., D820 g, N822K, Y823D, and A829P).

 

pKa: 11.84±0.70(Predicted)

 

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

 

Isomeric SMILES: CC1=C(C=C(C=N1)NC(=O)C2=CC(=C(C=C2)CN3CCN(CC3)C)C(F)(F)F)NC4=NC=CC(=N4)C5=CN=CC=C5  

 

InChIKey: BJCJYEYYYGBROF-UHFFFAOYSA-N  

 

InChI: InChI=1S/C29H29F3N8O/c1-19-26(38-28-34-9-7-25(37-28)21-4-3-8-33-16-21)15-23(17-35-19)36-27(41)20-5-6-22(24(14-20)29(30,31)32)18-40-12-10-39(2)11-13-40/h3-9,14-17H,10-13,18H2,1-2H3,(H,36,41)(H,34,37,38)

 

Attribute
[Chem Name]	4-[(4-methylpiperazin-1-yl)methyl]-N-[6-methyl-5-[(4-pyridin-3-ylpyrimidin-2-yl)amino]pyridin-3-yl]-3-(trifluoromethyl)benzamide
[Synonym]	Flumatinib; HH-GV-678
[CAS No.]	895519-90-1
[MDL No.]	MFCD18633213
[Formula]	C29H29F3N8O
[Molecular]	562.59
[Form]	A solid
[Storage]	Keep in dark place. Sealed in dry, 2-8°C

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