Opnurasib
Based on 7 publication(s) in Google Scholar
Opnurasib (JDQ-443) (NVP-JDQ443) is an orally active, potent, selective, and covalent KRAS G12C inhibitor. Opnurasib shows antitumor activity.
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: 98.20%
- CAS 番号: 2653994-08-0
- 分子式: C29H28ClN7O
- 分子量:526.03
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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
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
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MedChemExpress（MCE）の使用を引用している文献 Opnurasib
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生物活性
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KRas G12C |
Opnurasib traps the GDP-bound inactive conformation of KRAS[1].
Opnurasib promotes dose-dependent reductions of phosphorylated ERK (pERK) levels and the proliferation of the KRASG12C-mutated cell lines NCI-H358 and NCI-H2122, with IC50 values of 0.018 and 0.063 μM, respectively[2].
Opnurasib covalently and selectively binds and inhibits GDP-bound KRASG12C with low reversible binding affinity to the RAS switch II pocket, and also inhibits proliferation of KRASG12C-mutated and KRAS G12C/H95, G12C/R68S, and G12C/Y96 double-mutant cell lines[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ba/F3 cells
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Concentration:0, 0.3, 1 μM
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Incubation Time:30 min, 4 h
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Result:Inhibited signaling (pERK) and proliferation of the KRAS G12C/H95 double mutants G12C/H95R and G12C/H95Q.
Opnurasib (Orally, 100 mg/kg, daily (JDQ443) + 7.5 mg/kg, twice daily (TNO155), for 36 days) shows greater cell growth inhibition or cell killing compared with single-agent JDQ443 when combined with TNO155[2].
Opnurasib generates categorical antitumor responses in PDX models of NSCLC and colorectal tumors that are improved by combination treatment with other agents[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:KRAS G12C tumor-bearing nude mice (MIA PaCa-2 (PDAC); NCIH2122, LU99, HCC44, NCI-H2030 (NSCLC); and KYSE410 (esophageal cancer))[2]
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Dosage:10, 30, 100 mg/kg
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Administration:Orally, daily for 14 days
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Result:Inhibited the growth of all models in a dose-dependent manner.
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Animal Model:Three KRAS G12C-mutated CDX models (LU99, NCI-H2030, and KYSE410)[2]
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Dosage:100 mg/kg (JDQ443) + 7.5 mg/kg (TNO155)
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Administration:Orally, daily (JDQ443) or twice daily (TNO155), for 36 days
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Result:Combined with TNO155, showed either greater tumor efficacy compared with each agent alone (H2030, KYSE410) or a delayed time to tumor progression (LU99).
| 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 2653994-08-0
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性状 Solid
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分子量 526.03
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分子式 C29H28ClN7O
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Color White to off-white
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SMILES
O=C(C=C)N1CC2(C1)CC(N3N=C(C4=CC=C5C(C=NN5C)=C4)[C@]([C@]6=C(Cl)C(C)=CC7=C6C=NN7)=C3C)C2
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別名
JDQ-443; NVP-JDQ443
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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
Publications (7)
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Journal Impact Factor
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Most Recent
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Cell
2024 Oct 31;187(22):6379-6392.e17. PMID: 39255801 -
Cancer Discov
Sotorasib is a pan-RASG12C inhibitor capable of driving clinical response in NRASG12C cancers. [Abstract]2024 May 1;14(5):727-736. PMID: 38236605 -
Cancer Res
PRT3789 is a First-in-Human SMARCA2-Selective Degrader that Induces Synthetic Lethality in SMARCA4-Mutated Cancers. [Abstract]2025 Sep 24. PMID: 40991405 -
Biomed Pharmacother
ABCB1 attenuates brain exposure to the KRASG12C inhibitor opnurasib whereas binding to mouse carboxylesterase 1c influences its plasma exposure. [Abstract]2024 May 10:175:116720. PMID: 38733773 -
ACS Omega
Application and Cross-Validation of a High-Throughput SPR Method for Characterizing Covalent Binding Ligands. [Abstract]2025 Jul 4;10(27):29637-29646. PMID: 40687013 -
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溶剤 & 溶解度
DMSO : 80 mg/mL (152.08 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)
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: ≥ 2.08 mg/mL (3.95 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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.
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 (285 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. LIU BO, et al. PYRAZOLYL DERIVATIVES USEFUL AS ANTI-CANCER AGENTS. Patent WO2021120890A1.
[2]. Weiss A, Lorthiois E, Barys L, et al. Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent and Selective, Covalent Oral Inhibitor of KRASG12C. Cancer Discov. 2022;candisc.0158.2022. [Content Brief]
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 | 1.9010 mL | 9.5052 mL | 19.0103 mL | 47.5258 mL |
| 5 mM | 0.3802 mL | 1.9010 mL | 3.8021 mL | 9.5052 mL | |
| 10 mM | 0.1901 mL | 0.9505 mL | 1.9010 mL | 4.7526 mL | |
| 15 mM | 0.1267 mL | 0.6337 mL | 1.2674 mL | 3.1684 mL | |
| 20 mM | 0.0951 mL | 0.4753 mL | 0.9505 mL | 2.3763 mL | |
| 25 mM | 0.0760 mL | 0.3802 mL | 0.7604 mL | 1.9010 mL | |
| 30 mM | 0.0634 mL | 0.3168 mL | 0.6337 mL | 1.5842 mL | |
| 40 mM | 0.0475 mL | 0.2376 mL | 0.4753 mL | 1.1881 mL | |
| 50 mM | 0.0380 mL | 0.1901 mL | 0.3802 mL | 0.9505 mL | |
| 60 mM | 0.0317 mL | 0.1584 mL | 0.3168 mL | 0.7921 mL | |
| 80 mM | 0.0238 mL | 0.1188 mL | 0.2376 mL | 0.5941 mL | |
| 100 mM | 0.0190 mL | 0.0951 mL | 0.1901 mL | 0.4753 mL |
Opnurasib 関連分類
HY-139612 関連分類
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