MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報，我們不為任何個人用途提供產(chǎn)品和服務(wù)。

Opnurasib

產(chǎn)品活性：Opnurasib (JDQ-443) (NVP-JDQ443) 是一種口服有效和選擇性的共價 KRAS G12C 抑制劑。Opnurasib 具有抗腫瘤活性。

研究領(lǐng)域：GPCR/G Protein  |  Cell Cycle/DNA Damage

作用靶點：Ras  |  PERK

In Vitro: Opnurasib (NVP-JDQ443) traps the GDP-bound inactive conformation of KRAS.
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.
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.

In Vivo: Opnurasib (10-100 mg/kg, Orally, daily for 14 days) shows antitumor activity in KRAS G12C-mutated CDX models.
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.
Opnurasib generates categorical antitumor responses in PDX models of NSCLC and colorectal tumors that are improved by combination treatment with other agents.

相關(guān)產(chǎn)品：Drug Repurposing Compound Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Cell Cycle/DNA Damage Compound Library  |  GPCR/G Protein Compound Library  |  Kinase Inhibitor Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Ferroptosis Compound Library  |  Endoplasmic Reticulum Stress Compound Library  |  Orally Active Compound Library  |  Glutamine Metabolism Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Angiogenesis-Related Compound Library  |  Anti-Liver Cancer Compound Library   |  Anti-Colorectal Cancer Compound Library   |  Membrane Protein-targeted Compound Library  |  Membrane Receptor-targeted Compound Library  |  LC-2  |  KRAS G12C inhibitor 54  |  MRTX1133  |  AZA1  |  RBC10  |  CFL-137  |  Deltarasin hydrochloride  |  BDP9066  |  CCG-100602  |  KRAS inhibitor-4  |  KRas G12R inhibitor 1  |  MRTX0902  |  KRAS G12C inhibitor 25  |  Antitumor agent-60  |  KRAS G12C inhibitor 30  |  KRas G12C inhibitor 1  |  Spiclomazine hydrochloride  |  GGTI-286 hydrochloride  |  6H05  |  AZD4625  |  SOS1-IN-6  |  Antineoplaston A10  |  K-Ras-IN-1  |  BI-0474  |  Diazepinomicin  |  MK-28  |  K20  |  BQU57  |  KRAS G12D inhibitor 12

品牌介紹:
•   MCE (MedChemExpress) 擁有200 多種*僅有化合物庫，我們致力于為*科研客戶提供前沿的高品質(zhì)小分子活性化合物；
•   50,000 多種高選擇性抑制劑、激動劑涉及各熱門信號通路及疾病領(lǐng)；
•   產(chǎn)品種類涵蓋各種重組蛋白，多肽，常用試劑盒 ，更有 PROTAC、ADC 等特色產(chǎn)品，廣泛應(yīng)用于新藥研發(fā)、生命科學(xué)等科研項目；
•   提供虛擬篩選，離子通道篩選，代謝組學(xué)分析檢測分析，藥物篩選等專業(yè)技術(shù)服務(wù)；
•   設(shè)有專業(yè)的實驗中心和嚴格的質(zhì)控、驗證體系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各項質(zhì)檢報告，確保產(chǎn)品的高純度、高品質(zhì)；
•   產(chǎn)品的生物活性多經(jīng)各國客戶實驗驗證；
•   Nature, Cell, Science 等多種頂級期刊及制藥 Patent 收錄了MCE客戶的科研成果；
•   專業(yè)團隊跟蹤最新的制藥及生命科學(xué)研究進展，為您提供*新的活性化合物；
•   與世界各大制藥公司及著名科研機構(gòu)建立了長期的合作。