AMG410 diTFA
AMG410 diTFA is a non-covalent and selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 diTFA shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 diTFA is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 diTFA blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 diTFA can be used for the study of colorectal, pancreatic, and lung cancers.
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- CAS 番号: 3040175-18-3
- 分子式: C35H34ClF8N7O9
- 分子量:884.13
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
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KRas G12D 1-4 nM (IC50) |
KRas G12V 1-4 nM (IC50) |
AMG410 diTFA shows potent antiproliferative activity in KRAS-mutant cells (median IC50 = 12 nM). Importantly, AMG410 diTFA does not have antiproliferative activity in non-KRAS-transformed cells (median IC50 > 5 µM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 3040175-18-3
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分子量 884.13
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分子式 C35H34ClF8N7O9
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SMILES
FC1=C(C2=C(C=NN3)C3=CC(Cl)=C2CCCO4)N=CC5=C1N=C(OC[C@]67C[C@@H](F)CN6CCC7)N=C5N8CCOC[C@@H](OC4=O)C8.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)