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

BI-0474

  Cat. No.:  DC72237   Featured
Chemical Structure
2750570-55-7
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More than 5000 active chemicals with high quality for research!
Field of application
BI-0474 is a potent KRASG12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2750570-55-7
Chemical Name: BI-0474
Synonyms: Benzo[b]thiophene-3-carbonitrile, 2-amino-4-[3-[6-[(2S)-2,4-dimethyl-1-piperazinyl]-4-[4-(1-oxo-2-propen-1-yl)-1-piperazinyl]-2-pyridinyl]-1,2,4-oxadiazol-5-yl]-4,5,6,7-tetrahydro-4-methyl-, (4S)-;BI-0474
SMILES: C12CCC[C@@](C3ON=C(C4=NC(N5CCN(C)C[C@@H]5C)=CC(N5CCN(C(=O)C=C)CC5)=C4)N=3)(C)C=1C(C#N)=C(N)S2
Formula: C30H37N9O2S
M.Wt: 587.738883733749
Purity: 98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC72237 BI-0474 BI-0474 is a potent KRASG12C inhibitor with an IC50 value of 7.0 nM for the GDP-KRAS::SOS1 protein-protein interaction. BI-0474 exhibits good anti-proliferative activity against NCI-H358 cells carrying the G12C mutation. BI-0474 also shows good anti-tumour activity in non-small cell lung cancer xenograft models.
DC70234 AZD4625 AZD4625 is a potent, selective, covalent allosteric inhibitor of mutant GTPase KRAS G12C with IC50 of 3 nM, inhibitor H358 cell proliferation with GI50 of 4 nM.AZD4625 is a clinical development candidate for the treatment of KRASG12C positive tumors.
DC26136 MRTX849(Adagrasib) MRTX849(Adagrasib) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. MRTX849 covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bou
DC7344 ZCL 278 ZCL278 is a Cdc42 small molecule modulator that directly binds to Cdc42 (Kd=11.4 uM) and inhibits Cdc42-intersectin interaction.
DC8725 NSC 23766 NSC 23766 is a specific inhibitor of the binding and activation of Rac GTPase.
DC7467 ML-098 ML-098 is an activator of the GTP-binding protein Rab7 (EC50 = 77.6 nM) that demonstrates selectivity against the related GTPases cdc42, Ras, Rab-2A, and Rac1 (EC50s = 588.8, 346.7, 158.5, and 794.3 nM, respectively).
DC9906 K-Ras-IN-1 K-Ras-IN-1 is a K-Ras inhibitor, by binding to K-Ras in a hydrophobic pocket that is occupied by Tyr-71 in the apo-Ras crystal structure.
DC8816 ARS-853 ARS-853 is a selective, covalent inhibitor of KRAS-G12C that inhibits mutant KRAS driven signaling by binding to the GDP bound oncoprotein and preventing activation.
DC12031 ARS-1630 ARS-1630 is the R-conformational atropisomer of ARS-1620, 1,000-fold less potent than ARS-1620 (1.2 ± 0.6 M-1s-1) and thus acts as a unique inactive control compound..
DC10725 ARS-1620 ARS-1620 is a covalent compound with high potency and selectivity for KRAS-G12C.
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