Pan-RAS-IN-6
Pan-RAS-IN-6 (compound 24) is an inhibitor targeting DUSP6, which reduces MAPK activation in the brain of the NCI-H1373-Luc model (DUSP6), at the same time, it shows significant tumor growth inhibition and tumor regression effects in the NSCLC brain metastasis mouse model. Pan-RAS-IN-6 shows high selectivity and strong inhibitory effects, especially in KRAS mutation-related signaling pathways, demonstrating varying inhibitory activity against different KRAS mutants and interacting proteins. The IC50 values for KRAS G12C, G12D, and G12V are 1.3 nM, 4.7 nM, and 0.3 nM, respectively.
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- CAS 番号: 3054023-07-0
- 分子式: C46H60N8O5S
- 分子量:837.08
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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KRas G12C 1.3 nM (IC50) |
KRas G12D 4.7 nM (IC50) |
KRas G12V 0.3 nM (IC50) |
Pan-RAS-IN-6 inhibits the proliferation of NCI-H23, NCI-H358, NCI-H2444, RKN, and SW620 cells with IC50of 0.17 nM, 0.12 nM, 0.17 nM, 0.045 nM, and 0.1 nM[1].
Pan-RAS-IN-6 with the IC50 values against KRAS G12V, wild-type KRAS, wild-type HRAS, wild-type NRAS-BRAF, and CYPA interactions are 7 nM, 32 nM, 38 nM, and 35 nM, respectively; under G12C, G12D, and G12V conditions, the IC50 values for the KRAS-BRAF and CYPA interaction are 9.7 nM, 49.5 nM, and 7.1 nM, respectively; when inhibiting pERK, the IC50 values for both G12C and G12V are less than 0.6 nM, while for G12D, the IC50 is 0.9 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pan-RAS-IN-6 (30 mg/kg, p.o., once daily) reduces the expression of DUSP6 in the brain of the NCI-H1373-Luc model[1].
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 3054023-07-0
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分子量 837.08
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分子式 C46H60N8O5S
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SMILES
O=C(OCC(C)(C)CC1=[C@@]([C@@]2=C([C@@H](OC)C)N=CC(N3CCN(C)CC3)=C2)N4C5=C1C=C6C=C5CCC4)[C@H]7NN(C([C@@H](NC([C@H]8[C@H](C)[C@@H]8C)=O)CC9=NC6=CS9)=O)CCC7
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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)
Pan-RAS-IN-6 関連分類
HY-168012 関連分類
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