Name: EBI-907
Rating: 5 (10 reviews)

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HIT ID:HIT218963899
Cas No:1581764-31-9
常用名:EBI-907
IUPAC:N-(2-chloro-3-{1-cyclopropyl-8-methoxy-4H-pyrazolo[3,4-c]isoquinolin-7-yl}-4-fluorophenyl)-3-fluoropropane-1-sulfonamide
IUPAC:N-(2-chloro-3-{1-cyclopropyl-8-methoxy-4H-pyrazolo[3,4-c]isoquinolin-7-yl}-4-fluorophenyl)-3-fluoropropane-1-sulfonamide
InChI key:JSKJFDXTKYWPAH-UHFFFAOYSA-N

分子式:C23H21ClF2N4O3S
分子量:506.95
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:COc1cc2c3c(nnc3[nH]cc2cc1-c1c(F)ccc(NS(=O)(=O)CCCF)c1Cl)C1CC1
SMILES:COc1cc2c3c(nnc3[nH]cc2cc1-c1c(F)ccc(NS(=O)(=O)CCCF)c1Cl)C1CC1

EBI-907 is a highly potent and orally efficacious B-RafV600E inhibitor. EBI-907 displays a low single-digit nanomolar activity (IC50 = 4.9 nM), which is >10-fold more potent than Vemurafenib (IC50 = 59 nM). EBI-907 also exhibits high potency in selectively inhibiting the proliferation of BRAF (V600E)-dependent cell lines (A375 and Colo205) and cellular Erk phosporylation, with superior activity to Vemurafenib. EBI-907, displaying potent activity against a number of important oncogenic kinases including BRK, FGFR1, c-Kit, and PDGFRb.

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