Calderasib
Based on 1 Customer Validation
Calderasib (MK-1084) is a selective KRAS G12C inhibitor. Calderasib exhibits anticancer activity and can be used either alone or in combination with Pembrolizumab (HY-P9902) for cancer research.
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: 99.82%
- CAS 番号: 2641216-67-1
- 分子式: C32H31ClF2N6O4
- 分子量:637.08
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保管条件:
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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
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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
Calderasib (MK-1084) (0.01-10 μM, 2 h) inhibits the SOS-catalyzed nucleotide exchange with IC50 of 1.2 nM, inhibits the phosphorylation of ERK1/2 in cell H358 with IC50 of 9 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Calderasib (MK-1084) exhibits a good pharmacokinetic characteristics with a plasma clearance of 22 mL/min/kg, a mean residence time MRT of 1.1 h and an oral bioavailability of 61%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mouse MiaPaCa-2 xenograft models[2]
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Dosage:10-30 mg/kg
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Administration:po for 14 days
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Result:Inhibited tumor growth.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2641216-67-1
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性状 Solid
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分子量 637.08
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分子式 C32H31ClF2N6O4
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Color White to off-white
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SMILES
FC1=C2C(OCCOC3=CC=NC(C(C)C)=C3N4C5=NC2=C(Cl)C=C5C(N6[C@@H](C)CN(C(C=C)=O)[C@H](C)C6)=NC4=O)=C(F)C=C1
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別名
MK-1084
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
溶剤 & 溶解度
DMSO : 100 mg/mL (156.97 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 (stored under nitrogen). 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 (stored under nitrogen). 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 (279 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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 (stored under nitrogen). 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 |
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| DMSO | 1 mM | 1.5697 mL | 7.8483 mL | 15.6966 mL | 39.2415 mL |
| 5 mM | 0.3139 mL | 1.5697 mL | 3.1393 mL | 7.8483 mL | |
| 10 mM | 0.1570 mL | 0.7848 mL | 1.5697 mL | 3.9242 mL | |
| 15 mM | 0.1046 mL | 0.5232 mL | 1.0464 mL | 2.6161 mL | |
| 20 mM | 0.0785 mL | 0.3924 mL | 0.7848 mL | 1.9621 mL | |
| 25 mM | 0.0628 mL | 0.3139 mL | 0.6279 mL | 1.5697 mL | |
| 30 mM | 0.0523 mL | 0.2616 mL | 0.5232 mL | 1.3081 mL | |
| 40 mM | 0.0392 mL | 0.1962 mL | 0.3924 mL | 0.9810 mL | |
| 50 mM | 0.0314 mL | 0.1570 mL | 0.3139 mL | 0.7848 mL | |
| 60 mM | 0.0262 mL | 0.1308 mL | 0.2616 mL | 0.6540 mL | |
| 80 mM | 0.0196 mL | 0.0981 mL | 0.1962 mL | 0.4905 mL | |
| 100 mM | 0.0157 mL | 0.0785 mL | 0.1570 mL | 0.3924 mL |
Calderasib 関連分類
HY-162431 関連分類
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