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基本描述
| 英文名称 | opnurasib |
|---|---|
| 别名 | compound 5;example 1a;JDQ 443;JDQ-443;JDQ443;Nvp-jdq443 |
| 英文别名 | compound 5;example 1a;JDQ 443;JDQ-443;JDQ443;Nvp-jdq443 |
名称和标识符
| IUPAC Name | 1-[6-[4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methylindazol-5-yl)pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl]prop-2-en-1-one |
|---|---|
| INCHI | InChI=1S/C29H28ClN7O/c1-5-24(38)36-14-29(15-36)10-20(11-29)37-17(3)25(26-21-13-31-33-22(21)8-16(2)27(26)30)28(34-37)18-6-7-23-19(9-18)12-32-35(23)4/h5-9,12-13,20H,1,10-11,14-15H2,2-4H3,(H,31,33) |
| InChi Key | AZUYLZMQTIKGSC-UHFFFAOYSA-N |
| Canonical SMILES | CC1=CC2=C(C=NN2)C(=C1Cl)C3=C(N(N=C3C4=CC5=C(C=C4)N(N=C5)C)C6CC7(C6)CN(C7)C(=O)C=C)C |
| 关联CAS | 2653994-08-0 |
| PubChem CID | 156501355 |
| MeSH Entry Terms | 1-(6-(4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methylindazol-5-yl)pyrazol-1-yl)-2-azaspiro(3.3)heptan-2-yl)prop-2-en-1-one;JDQ443 |
数据库链接
| PubChem CID | 156501355 |
|---|---|
| CAS Registry No. | 2653994-08-0 |
关联配体
| Ligand ID | 11715 |
|---|---|
| 名称 | opnurasib |
| 别名 | JDQ-443 |
| 类别 | Synthetic organic |
| 学名 | 1-[6-[4-(5-chloro-6-methyl-1H-indazol-4-yl)-5-methyl-3-(1-methylindazol-5-yl)pyrazol-1-yl]-2-azaspiro[3.3]heptan-2-yl]prop-2-en-1-one |
| 生物活性评价 |
The sulfonamide class of antibacterial compounds are primarily bacteriostatic agents and have a broad spectrum of activity against both Gram-positive and Gram-negative species of bacteria (reviewed in |
| 评价 |
Opnurasib (JDQ443) is a clinical stage, covalent KRASG12C inhibitor that is being developed by Novartis for anti-tumour potential. We obtained this structure from a list compiled by DrugHunter of first time disclosures made at the 2021 XXVI EFMC International Symposium on Medicinal Chemistry (EFMC-ISMC). This chemical structure was submitted to PubChem by SureChEMBL in August 2021, and is likely to have originated from a patent extraction. The compound's discovery was published in June 2022 |
| 临床描述 |
This is a phase Ib/II open label study. The escalation part will characterize the safety and
tolerability of JDQ443 single agent and JDQ443 in combination with the other study treatments
(TNO155 and spartalizumab) in advanced solid tumor patients. After the determination of the
maximum tolerated dose / recommended dose for a particular treatment arm, dose expansion will
assess the anti-tumor activity and further assess the safety, tolerability, and PK/PD of each
regimen at the maximum tolerated dose / recommended dose.
This is Phase Ib/II, multicenter, open-label adaptive platform study of JDQ443 with select therapies in patients with advanced solid tumors harboring the KRAS G12C mutation. This is a phase III open label study designed to compare JDQ443 as monotherapy to docetaxel in participants with advanced non-small cell lung cancer (NSCLC) harboring a KRAS G12C mutation who have been previously treated with a platinum-based chemotherapy and immune checkpoint inhibitor therapy either in sequence or in combination. |
| 来源公司 |
Novartis Novartis Novartis |
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参考文献
| 1. Weiss A, Lorthiois E, Barys L, Beyer KS, Bomio-Confaglia C, Burks H, Chen X, Cui X, de Kanter R, Dharmarajan L et al.. (2022) Discovery, Preclinical Characterization, and Early Clinical Activity of JDQ443, a Structurally Novel, Potent, and Selective Covalent Oral Inhibitor of KRASG12C.. Cancer Discov, 12 (6): (1500-1517). [PMID:35404998] |
| 2. Lorthiois E, Gerspacher M, Beyer KS, Vaupel A, Leblanc C, Stringer R, Weiss A, Wilcken R, Guthy DA, Lingel A et al.. (2022) JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors.. J Med Chem, 71 (13): (1755-70). [PMID:36399068] |
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