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Home > Inhibitors & Agonists > Ras-Raf-MAPK-ERK > Raf

B-Raf inhibitor 1

  Cat. No.:  DC8921   Featured
Chemical Structure
1093100-40-3
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More than 5000 active chemicals with high quality for research!
Field of application
B-Raf inhibitor 1 is a potent and selective B-Raf inhibitor with cell IC50s of 0.31 uM and 2 nM for A375 proliferation and A375 p-ERK respectively.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 1093100-40-3
Chemical Name: B-Raf inhibitor 1
Synonyms: N1-(4-chlorophenyl)-6-methyl-N5-[3-(9H-purin-6-yl)-2-pyridinyl]-1,5-Isoquinolinediamine;B-Raf inhibitor 1;1,5-Isoquinolinediamine, N1-(4-chlorophenyl)-6-methyl-N5-[3-(9H-purin-6-yl)-2-pyridinyl]-;1-N-(4-chlorophenyl)-6-methyl-5-N-[3-(7H-purin-6-yl)pyridin-2-yl]isoquinoline-1,5-diamine;N5-(3-(9H-purin-6-yl)pyridin-2-yl)-N1-(4-chlorophenyl)-6-methylisoquinoline-1,5-diamine;N~1~-(4-Chlorophenyl)-6-Methyl-N~5~-[3-(7h-Purin-6-Yl)pyridin-2-Yl]isoquinoline-1,5-Diamine;B-Rafinhibitor1;3idp;B-raf;B-Raf inhibitor1;BDBM35327;pyr;L1E;pyrid;Raf inhibitor 1
SMILES: ClC1C([H])=C([H])C(=C([H])C=1[H])N([H])C1C2C([H])=C([H])C(C([H])([H])[H])=C(C=2C([H])=C([H])N=1)N([H])C1=C(C([H])=C([H])C([H])=N1)C1=C2C(=NC([H])=N1)N=C([H])N2[H]
Formula: C26H19ClN8
M.Wt: 478.9357
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: B-Raf inhibitor 1 is a potent Raf kinase inhibitor with Kis of 1 nM, 1 nM, and 0.3 nM for B-RafWT, B-RafV600E, and C-Raf, respectively.
In Vitro: B-Raf inhibitor 1 (Compound 13) inhibits A375 and HCT-116 proliferation with IC50s of 0.31 and 0.72 μM, respectively. B-Raf inhibitor 1 (Compound 13) binds to and stabilizes B-Raf in a DFG-out, inactive conformation in which the ATP pocket is partially filled by Phe595 and Gly596 from the DFG motif. B-Raf inhibitor 1 (Compound 13) additionally exhibits low micromolar inhibition against wild type B-Raf cell lines, which may be due to off-target kinase activities or alternatively to pan-Raf inhibition, including Raf dimers[1].
References: [1]. Wang X, et al. Conformation-specific effects of Raf kinase inhibitors. J Med Chem. 2012 Sep 13;55(17):7332-41.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
Cat. No. Product name Field of application
DC47985 GNE-9815 GNE-9815 is among the most highly kinase-selective RAF inhibitors targeting KRAS mutant cancers via combination treatment.
DC7719 ZM336372 ZM 336372 is a potent and selective c-Raf inhibitor with IC50 of 70 nM, 10-fold selectivity over B-RAF, no inhibition to PKA/B/C, AMPK, p70S6, etc.
DC7307 TAK-632 TAK-632 is a selective pan-RAF kinase inhibitor with IC50 values of 2.4/1.4 nM for BRAF V600E/c-RAF; > 60 fold selectivity over VEGFR.
DC8791 Sorafenib free base (BAY-43-9006) Sorafenib(BAY 43-9006) is a potent inhibitor of Raf-1 with IC50 values of 6 nM, 22 nM and 90 nM for Raf-1, B-Raf, and VEGFR2 respectively, BAY 43-9006 suppresses both wild-type and V599E mutant BRAF activity in vitro.
DC2098 Sorafenib (BAY-43-9006) Sorafenib Tosylate (Bay 43-9006, Nexavar) is a multikinase inhibitor of Raf-1, B-Raf and VEGFR-2 with IC50 of 6 nM, 22 nM and 90 nM, respectively.
DC7279 SB-590885 SB590885 is a potent B-Raf inhibitor with Ki of 0.16 nM, 11-fold greater selectivity for B-Raf over c-Raf, no inhibition to other human kinases.
DC9987 RAF709 RAF709 is a novel Raf kinase inhibitor extracted from patent WO2014151616A1, compound example 131, has an IC50 of 0.5 and 1.8 nM for c-Raf and b-Raf, respectively.
DC5049 RAF265 (CHIR-265) RAF265 (CHIR-265) is a highly selective B-Raf and VEGFR2 inhibitor with IC50 of 3-60 nM and EC50 of 30 nM, including B-Raf, C-Raf and mutant B-Raf.
DC9814 PLX7904(PB04) PLX7904(PB04) is a potent and selective paradox-breaker RAF inhibitor.
DC6301 PLX-4720 PLX4720 is a potent and selective inhibitor of B-RafV600E with IC50 of 13 nM, equally potent to c-Raf-1(Y340D and Y341D mutations), 10-fold selectivity for B-RafV600E than wild-type B-Raf.
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