(7R)-Elisrasib
Based on 1 Customer Validation
KRASG12C IN-2 (compound 17) is an orally active KRASG12C inhibitor. KRASG12C IN-2 inhibits tumor growth in mice.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.52%
- CAS 番号: 2706637-12-7
- 分子式: C32H35F6N7O3
- 分子量:679.66
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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
生物活性
KRASG12C[1].
KRASG12C IN-2 (0-100 nM; 72 h) inhibits the inhibition of the proliferation of KRASG12C mutant MIA-PA-CA-2 cells, with an IC50 value of 0.44 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MIA-PA-CA-2 cells (with KRASG12C mutant)
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Concentration:0-100 nM
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Incubation Time:72 h
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Result:Exhibited antiproliferation activity (IC50 = 0.44 nM).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Nude Balb/c mice (Subcutaneous transplantation model of Mia PaCa-2 cells)[1].
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Dosage:10, 30 mg/kg
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Administration:Oral administration; single daily for 22 days.
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Result:Inhibited tumor growth in mice, and the inhibition rates are 93.06% (dosage at 10 mg/kg) and 99.64% (dosage at 30 mg/kg), respectively.
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Animal Model:Male SD rats and male CD mice[1].
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Dosage:2.0 mg/kg
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Administration:i.v.; single
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Result:
1.19 Pharmacokinetic Parameters of KRASG12C IN-2 in Male SD rats and Male CD mice[1].
Male SD rats Male CD mice IV (2 mg/kg) IV (2 mg/kg) T1/2 (h) 1.9 1.7 CL (mL/min/kg) 71.5 40.6 Vdss/Vdss, u(L/kg) 10.6/221 3.9/32.3 AUC0-last/AUCu (nM•h) 653/31.3 1297/155.6
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Animal Model:Male SD rats and male CD mice[1].
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Dosage:9.8, 10.3 mg/kg
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Administration:p.o.; single
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Result:
1.19 Pharmacokinetic Parameters of KRASG12C IN-2 in Male SD rats and Male CD mice[1].
Male SD rats Male CD mice PO (9.8 mg/kg) PO (10.3 mg/kg) AUC0-last/AUCu (nM•h) 995/47.8 1422/170.6 Tmax (h) 1.5 1.0 Cmax/Cmax, u (nM) 220/10.6 431/51.7 F (%) 30.5% 21.9%
化学情報
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CAS 番号 2706637-12-7
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性状 Solid
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分子量 679.66
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分子式 C32H35F6N7O3
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Color White to off-white
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SMILES
FC(F)(F)C(C(C)=CC(N)=C1F)=C1[C@H]2CC3=NC(OC[C@@]45N(CCC5)C[C@@H](C4)F)=NC(N6C[C@@H](N(CC6)C(C(F)=C)=O)CC#N)=C3CO2
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別名
(7R)-D3S-001
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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
純度とドキュメンテーション
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データシート (279 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
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)