RM-018
Based on 1 Customer Validation
RM-018 is a potent, functionally distinct tricomplex KRASG12C active-state inhibitor. RM-018 retains the ability to bind and inhibit KRASG12C/Y96D and could overcome resistance. RM-018 binds specifically to the GTP-bound, active [“RAS(ON)”] state of KRASG12C.
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- 純度: 95.95%
- CAS 番号: 2641993-55-5
- 分子式: C56H72N8O8
- 分子量:985.22
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 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) |
KRAS (G12C/Y96D) |
RM-018 is a “tricomplex” KRAS inhibitor, which exploits a highly abundant chaperone protein, cyclophilin A, to bind and inhibit KRASG12C[1].
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RM-018 (0.01-1000 nM; 72 hours) has IC50s of 1.4-3.5 nM (KRASG12C) and 2.8-7.3 nM (KRASG12C/Y96D) in NCI-H358, MIA PaCa-2, Ba/F3, and MGH1138-1 cells[1].
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RM-018 (0-100 nM; 4 hours) inhibits the expression of KRAS, pERK, and pRSK protein[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H358, MIA PaCa-2, Ba/F3, and MGH1138-1 cells, which stably infected with KRASG12C or KRASG12C/Y96D.
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Concentration:0.01-1000 nM
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Incubation Time:72 hours
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Result:Inhibited the cell activity, but largely unaffected by KRASG12C/Y96D expression.
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Cell Line:MIA PaCa-2, HEK293T and MGH1138-1 cells, which expressing KRASG12C or KRASG12C/Y96D.
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Concentration:0-100 nM
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Incubation Time:4 hours
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Result:Inhibited KRAS, pERK and pRSK levels with similar potency.
化学情報
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CAS 番号 2641993-55-5
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性状 Solid
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分子量 985.22
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分子式 C56H72N8O8
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Color Off-white to light yellow
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SMILES
O=C(N1CCC[C@@H](C(OCC(C)(C)CC2=[C@@]([C@@]3=C([C@H](C)OC)N=CC=C3)N(CC)C4=C2C=C5C=C4)=O)N1)[C@@H](NC([C@H](C(C)C)N(C)C([C@H]6CCN(C(C#CCN7CCOCC7)=O)C6)=O)=O)CC8=CC=CC5=C8
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 60 mg/mL (60.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (274 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.0150 mL | 5.0750 mL | 10.1500 mL | 25.3750 mL |
| 5 mM | 0.2030 mL | 1.0150 mL | 2.0300 mL | 5.0750 mL | |
| 10 mM | 0.1015 mL | 0.5075 mL | 1.0150 mL | 2.5375 mL | |
| 15 mM | 0.0677 mL | 0.3383 mL | 0.6767 mL | 1.6917 mL | |
| 20 mM | 0.0508 mL | 0.2538 mL | 0.5075 mL | 1.2688 mL | |
| 25 mM | 0.0406 mL | 0.2030 mL | 0.4060 mL | 1.0150 mL | |
| 30 mM | 0.0338 mL | 0.1692 mL | 0.3383 mL | 0.8458 mL | |
| 40 mM | 0.0254 mL | 0.1269 mL | 0.2538 mL | 0.6344 mL | |
| 50 mM | 0.0203 mL | 0.1015 mL | 0.2030 mL | 0.5075 mL | |
| 60 mM | 0.0169 mL | 0.0846 mL | 0.1692 mL | 0.4229 mL |
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