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Opnurasib
🥰Excellent
Catalog No. T40292Cas No. 2653994-08-0
Alias Opnurasib, NVP-JDQ443, JDQ-443
Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small cell lung cancer.
Opnurasib
🥰Excellent
Purity: 98.88%
Catalog No. T40292Alias Opnurasib, NVP-JDQ443, JDQ-443Cas No. 2653994-08-0
Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small cell lung cancer.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | 101 € | In Stock | |
| 5 mg | 353 € | In Stock | |
| 10 mg | 527 € | In Stock | |
| 25 mg | 848 € | In Stock | |
| 50 mg | Inquiry | In Stock | |
| 1 mL x 10 mM (in DMSO) | 406 € | In Stock |
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View MoreInhibitors Related to "Opnurasib"
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MRTX1133 is a KRAS G12D inhibitor (KD=0.2 pM) that is potent, selective, and non-covalent. MRTX1133 exhibits inhibitory activity against KRAS G12D-mutated tumors, but not against KRAS wild-type tumors.
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Sotorasib
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AMG-510
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Sotorasib (AMG-510) is an orally active and selective covalent inhibitor of KRAS G12C. Sotorasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Sotorasib exhibits inhibitory activity against KRAS G12C mutant tumors.
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Adagrasib Cited
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Adagrasib (MRTX849) is an orally active and selective covalent inhibitor of KRAS G12C. Adagrasib binds to the GDP state of the inactive conformation of KRAS G12C and inhibits KRAS and its downstream signaling. Adagrasib exhibits inhibitory activity against KRAS G12C mutant tumors.
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Cited(S)-AMG-510
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(S)-AMG-510 is the S-type compound of AMG-510 (Sotorasib), which effectively and selectively inhibits KRASG12C through covalent interaction with mutant cysteine, thereby promoting clinical efficacy in KRASG12C tumors.
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GNE-9815
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BI-3406 Cited
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MRTX-1257
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MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C with an IC50 of 900 pM for KRAS-dependent ERK phosphorylation in H358 cells. MRTX-1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above cellular potency, and 77% target engagement in a PK/PD experiment.
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Purity:98.88%
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All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.Product Introduction
Bioactivity
Chemical Properties
| Description | Opnurasib (JDQ-443) is an orally available and selective and potent covalent KRAS G12C inhibitor with antitumor activity for the study of advanced non-small cell lung cancer. |
| In vitro | Opnurasib selectively forms a covalent bond with and inhibits GDP-bound KRASG12C, demonstrating a low reversible binding affinity to the RAS switch II pocket. Additionally, it effectively hinders the proliferation of cell lines carrying KRASG12C mutations, as well as those with double mutations G12C/H95, G12C/R68S, and G12C/Y96.[2] Opnurasib induces dose-dependent decreases in phosphorylated ERK (pERK) levels and inhibits the proliferation of KRASG12C-mutated cell lines NCI-H358 and NCI-H2122, exhibiting IC50 values of 0.018 and 0.063 μM, respectively.[2] |
| In vivo | Opnurasib elicits distinct antitumor responses in patient-derived xenograft (PDX) models of non-small cell lung cancer (NSCLC) and colorectal tumors, and these responses are further enhanced when Opnurasib is used in combination with other therapeutic agents.[2] |
| Alias | Opnurasib, NVP-JDQ443, JDQ-443 |
| Molecular Weight | 526.03 |
| Formula | C29H28ClN7O |
| Cas No. | 2653994-08-0 |
| Smiles | Cc1c(c(nn1C1CC2(C1)CN(C2)C(=O)C=C)-c1ccc2n(C)ncc2c1)-c1c(Cl)c(C)cc2[nH]ncc12 |
| Relative Density. | 1.46 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 70 mg/mL (133.07 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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