MRTX-1257
Based on 5 publication(s) in Google Scholar
MRTX-1257 is a selective, irreversible, covalent and orally active KRAS G12C inhibitor, with an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells.
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: 99.71%
- CAS 番号: 2206736-04-9
- 分子式: C33H39N7O2
- 分子量:565.71
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保管条件:
-20°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
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生物活性
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KRAS(G12C) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H358 | IC50 |
1 nM
Compound: 19
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Inhibition of KRAS G12C mutant in human NCI-H358 cells assessed as reduction in ERK phosphorylation incubated for 3 hrs by in-cell western method
Inhibition of KRAS G12C mutant in human NCI-H358 cells assessed as reduction in ERK phosphorylation incubated for 3 hrs by in-cell western method
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[PMID: 32250617] |
MRTX-1257 shows sustained regression at 3,10, 30, and 100 mg/kg dose groups[1].
MRTX-1257 dosed of 100 mg/kg daily leads to complete responses that are maintained >70 days after cessation of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MIA PaCa-2 G12C Xenograft Model (mouse)[1].
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Dosage:1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg.
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Administration:Orally daily for 30 days.
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Result:Showed rapid tumor growth inhibition at all dose groups.
Showed sustained regression at 3,10, 30, and 100 mg/kg dose groups.
100 mg/kg daily led to complete responses that are maintained >70 days after cessation of treatment.
化学情報
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CAS 番号 2206736-04-9
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性状 Solid
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分子量 565.71
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分子式 C33H39N7O2
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Color Off-white to light yellow
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SMILES
N#CC[C@@H]1N(C(C=C)=O)CCN(C2=C3C(CN(C4=C5C(C)=CC=CC5=CC=C4)CC3)=NC(OC[C@H]6N(C)CCC6)=N2)C1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Publications (5)
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Journal Impact Factor
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Most Recent
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J Am Chem Soc
2022 Sep 28;144(38):17432-17440. PMID: 36122391 -
Cell Chem Biol
2026 Feb 11:S2451-9456(26)00027-9. PMID: 41679298 -
J Proteome Res
2021 Dec 3;20(12):5379-5391. PMID: 34751028 -
Biomed Chromatogr
Development and validation of an ultra-performance liquid chromatography-tandem mass spectrometry method to quantify the small molecule inhibitors adagrasib, alectinib, brigatinib, capmatinib, crizotinib, lorlatinib, selpercatinib, and sotorasib in human plasma. [Abstract]2024 Oct;38(10):e5986. PMID: 39136165 -
溶剤 & 溶解度
DMSO : 55 mg/mL (97.22 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.42 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.42 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (278 KB)
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- Korean - KR (393 KB)
- Portuguese - PT (393 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7677 mL | 8.8385 mL | 17.6769 mL | 44.1923 mL |
| 5 mM | 0.3535 mL | 1.7677 mL | 3.5354 mL | 8.8385 mL | |
| 10 mM | 0.1768 mL | 0.8838 mL | 1.7677 mL | 4.4192 mL | |
| 15 mM | 0.1178 mL | 0.5892 mL | 1.1785 mL | 2.9462 mL | |
| 20 mM | 0.0884 mL | 0.4419 mL | 0.8838 mL | 2.2096 mL | |
| 25 mM | 0.0707 mL | 0.3535 mL | 0.7071 mL | 1.7677 mL | |
| 30 mM | 0.0589 mL | 0.2946 mL | 0.5892 mL | 1.4731 mL | |
| 40 mM | 0.0442 mL | 0.2210 mL | 0.4419 mL | 1.1048 mL | |
| 50 mM | 0.0354 mL | 0.1768 mL | 0.3535 mL | 0.8838 mL | |
| 60 mM | 0.0295 mL | 0.1473 mL | 0.2946 mL | 0.7365 mL | |
| 80 mM | 0.0221 mL | 0.1105 mL | 0.2210 mL | 0.5524 mL |
MRTX-1257 関連分類
HY-114436 関連分類
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