{"id":54968,"date":"2026-08-04T14:37:20","date_gmt":"2026-08-04T06:37:20","guid":{"rendered":"https:\/\/biopioneer.com.tw\/?p=54968"},"modified":"2026-08-04T14:40:41","modified_gmt":"2026-08-04T06:40:41","slug":"kras-g12c-%e6%8a%91%e5%88%b6%e5%8a%91-adagrasib-mrtx849-cas-2326521-71-3-selleck%e8%b2%a8%e8%99%9f-s8884","status":"publish","type":"post","link":"https:\/\/biopioneer.com.tw\/?p=54968","title":{"rendered":"KRAS G12C \u6291\u5236\u5291-Adagrasib (MRTX849) | CAS# 2326521-71-3 Selleck\u8ca8\u865f S8884"},"content":{"rendered":"
\n

Selleck chemicals \u7cfb\u5217\u5546\u54c1->><\/span><\/span><\/span><\/span><\/strong>KRas \u6291\u5236\u5291\/Adagrasib (MRTX849)<\/span><\/span><\/span><\/span><\/p>\n

Adagrasib (MRTX849) \u662f\u4e00\u7a2e\u5f37\u6548\u3001\u9078\u64c7\u6027\u7684\u5171\u50f9 KRAS G12C \u6291\u5236\u5291\u3002\u5b83\u900f\u904e\u8207\u7a81\u8b8a\u578b KRAS \u86cb\u767d\u7684 Cys12 \u4f4d\u9ede\u5171\u50f9\u7d50\u5408\uff0c\u5f71\u97ff KRAS\/MAPK\/ERK \u8a0a\u865f\u901a\u8def\uff0c\u5f9e\u800c\u6709\u6548\u6291\u5236 KRAS \u4f9d\u8cf4\u6027\u8a0a\u865f\u50b3\u5c0e\uff0c\u4e26\u6291\u5236\u764c\u7d30\u80de\u7684\u6d3b\u529b\u8207\u589e\u6b96\u3002<\/p>\n

KRAS G12C \u6291\u5236\u5291-Adagrasib (MRTX849) | CAS# 2326521-71-3 Selleck\u8ca8\u865f S8884<\/a><\/span><\/p>\n

Adagrasib (MRTX849) is a potent, selective, and covalent KRAS G12C inhibitor. It affects the KRAS\/MAPK\/ERK signaling pathways by covalently binding to the mutant KRAS protein at Cys12, effectively inhibiting KRAS-dependent signal transduction and suppressing cancer cell viability and proliferation.<\/p>\n

\u7522\u54c1\u4ecb\u7d39<\/span><\/strong><\/span><\/p>\n

<\/p>\n

\u975e\u5c0f\u7d30\u80de\u80ba\u764c\uff1aAdagrasib (MRTX849) \u5fb9\u5e95\u6539\u8b8a\u4e86\u651c\u5e36KRAS G12C\u7a81\u8b8a\u7684\u975e\u5c0f\u7d30\u80de\u80ba\u764c\u7684\u6cbb\u7642\u6a21\u5f0f\u3002\u5927\u91cf\u81e8\u5e8a\u8a66\u9a57\u5df2\u8b49\u5be6\uff0c\u7121\u8ad6\u4f5c\u70ba\u55ae\u85e5\u6cbb\u7642\u6216\u8207\u514d\u75ab\u6aa2\u67e5\u9ede\u6291\u5236\u5291\uff08\u5982\u5e15\u535a\u5229\u73e0\u55ae\u6297\uff09\u806f\u5408\u6cbb\u7642\uff0cAdagrasib (MRTX849) \u5747\u5177\u6709\u986f\u8457\u7642\u6548\u548c\u826f\u597d\u7684\u5b89\u5168\u6027\u3002\u7814\u7a76\u4eba\u54e1\u6b63\u5728\u7a4d\u6975\u63a2\u7d22\u5176\u7a7f\u900f\u8840\u8166\u5c4f\u969c\u7684\u80fd\u529b\uff0c\u4ee5\u6cbb\u7642\u4e2d\u6a1e\u795e\u7d93\u7cfb\u7d71\u8f49\u79fb\u2014\u2014\u9019\u662f\u665a\u671f\u80ba\u764c\u5e38\u200b\u200b\u898b\u7684\u4f75\u767c\u75c7\u3002\u76ee\u524d\u7684\u7814\u7a76\u65e8\u5728\u5c07Adagrasib (MRTX849) \u78ba\u7acb\u70ba\u7b2c\u4e00\u7dda\u6cbb\u7642\u65b9\u6848\uff0c\u5f9e\u800c\u986f\u8457\u63d0\u9ad8\u651c\u5e36\u8a72\u7279\u5b9a\u57fa\u56e0\u7a81\u8b8a\u60a3\u8005\u7684\u7121\u60e1\u5316\u5b58\u6d3b\u671f\u548c\u7e3d\u5b58\u6d3b\u671f\u3002\u5728\u5927\u8178\u76f4\u8178\u764c\u9818\u57df\uff0cAdagrasib (MRTX849) \u5c55\u73fe\u51fa\u4ee4\u4eba\u9f13\u821e\u7684\u81e8\u5e8a\u6d3b\u6027\uff0c\u5c24\u5176\u662f\u5728\u806f\u5408\u6cbb\u7642\u4e2d\u3002\u7531\u65bc\u5927\u8178\u76f4\u8178\u816b\u7624\u5e38\u900f\u904e\u8868\u76ae\u751f\u9577\u56e0\u5b50\u53d7\u9ad4\uff08EGFR\uff09\u8a0a\u865f\u8def\u5f91\u7684\u91cd\u65b0\u6d3b\u5316\u800c\u5c0dKRAS\u6291\u5236\u5291\u7522\u751f\u6297\u85e5\u6027\uff0c\u56e0\u6b64Adagrasib (MRTX849) \u8207\u897f\u59a5\u6614\u55ae\u6297\uff08cetuximab\uff09\u7684\u806f\u5408\u6cbb\u7642\u5df2\u6210\u70ba\u4e3b\u8981\u7684\u7814\u7a76\u65b9\u5411\u3002\u9019\u7a2e\u5354\u540c\u7642\u6cd5\u5728\u5148\u524d\u63a5\u53d7\u904e\u5927\u91cf\u6cbb\u7642\u7684\u60a3\u8005\u4e2d\u53d6\u5f97\u4e86\u8f03\u9ad8\u7684\u5ba2\u89c0\u7de9\u89e3\u7387\u548c\u9577\u671f\u7684\u75be\u75c5\u63a7\u5236\u3002\u8fd1\u671f\u76e3\u7ba1\u6a5f\u69cb\u5c0d\u6b64\u806f\u5408\u7642\u6cd5\u7684\u6279\u51c6\u9032\u4e00\u6b65\u63a8\u52d5\u4e86\u514b\u670d\u9069\u61c9\u6027\u6297\u85e5\u6027\u6a5f\u5236\u548c\u512a\u5316\u665a\u671f\u5927\u8178\u76f4\u8178\u764c\u6cbb\u7642\u9806\u5e8f\u7684\u7814\u7a76\u3002\u9664\u4e86\u80ba\u764c\u548c\u5927\u8178\u76f4\u8178\u764c\u4e4b\u5916\uff0cAdagrasib (MRTX849) \u5728\u80f0\u817a\u5c0e\u7ba1\u817a\u764c\u548c\u5176\u4ed6\u651c\u5e36KRAS G12C\u7a81\u8b8a\u7684\u80c3\u8178\u9053\u816b\u7624\u4e2d\u7684\u6cbb\u7642\u6f5b\u529b\u4e5f\u6b63\u5728\u88ab\u5ee3\u6cdb\u8a55\u4f30\u3002\u9019\u4e9b\u764c\u75c7\u4ee5\u5f80\u88ab\u8a8d\u70ba\u7121\u6cd5\u6210\u85e5\uff0c\u9810\u5f8c\u6975\u5dee\uff0c\u4f46\u5728\u65e9\u671f\u81e8\u5e8a\u8a66\u9a57\u4e2d\uff0cAdagrasib (MRTX849) \u55ae\u85e5\u6cbb\u7642\u986f\u793a\u51fa\u4ee4\u4eba\u9f13\u821e\u7684\u5ba2\u89c0\u7de9\u89e3\u7387\u3002\u76ee\u524d\uff0c\u7814\u7a76\u4eba\u54e1\u6b63\u81f4\u529b\u65bc\u64f4\u5927\u9019\u4e9b\u968a\u5217\uff0c\u4ee5\u66f4\u597d\u5730\u4e86\u89e3\u7642\u6548\u7684\u6301\u4e45\u6027\u548c\u5b89\u5168\u6027\u3002\u6b64\u5916\uff0c\u7814\u7a76\u4e5f\u6b63\u5728\u63a2\u7d22\u5408\u7406\u7684\u5408\u4f75\u7528\u85e5\u7b56\u7565\uff0c\u4ee5\u63d0\u9ad8\u7642\u6548\u4e26\u5ef6\u7de9\u9019\u4e9b\u9ad8\u5ea6\u4fb5\u8972\u6027\u5be6\u9ad4\u816b\u7624\u7372\u5f97\u6027\u6297\u85e5\u6027\u7684\u767c\u751f\u3002<\/p>\n<\/div>\n

\n
\n\n\n\n\n\n\n\n\n
Storage<\/td>\n
M.Wt<\/td>\n604.12<\/td>\n<\/tr>\n
Cas No.<\/td>\n2326521-71-3<\/td>\n<\/tr>\n
Formula<\/td>\nC32<\/sub>H35<\/sub>ClFN7<\/sub>O2<\/sub><\/td>\n<\/tr>\n
Synonyms<\/td>\n<\/td>\n<\/tr>\n
Solubility<\/td>\nDMSO : 100 mg\/mL (165.53 mM)
\n(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)Ethanol : 100 mg\/mLWater : Insoluble<\/p>\n

The solubility data above are all experimental results (not literature values).<\/p>\n<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<\/div>\n<\/div>\n

<\/div>\n
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\"\u7db2\u7ad9\u898f\u683c\u5c0f\u5716_\u5de5\u4f5c\u5340\u57df<\/a><\/div>\n
<\/div>\n
\n\n\n\n\n\n\n\n\n
Product Name<\/strong><\/td>\nKey Target<\/strong><\/td>\nIC50<\/sub><\/strong><\/td>\nApplications<\/strong><\/td>\nStrengths<\/strong><\/td>\nLimitations<\/strong><\/td>\n<\/tr>\n<\/thead>\n
Daraxonrasib (RMC-6236)<\/strong><\/a><\/td>\npan-RAS \/ RAS(ON)<\/td>\n—<\/td>\nTreatment of patients with multiple RAS-addicted cancers, including pancreatic ductal adenocarcinoma (PDAC) and non-small cell lung cancer (NSCLC).<\/td>\nBroad-spectrum RAS inhibition with generally controllable side effects and effective tolerance by most patients.<\/td>\nThe potential for broad RAS inhibition to disrupt normal tissue homeostasis remains a significant concern.<\/td>\n<\/tr>\n
AMG 510 (Sotorasib)<\/strong><\/a><\/td>\nKRAS G12C<\/td>\n—<\/td>\nTreatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) with KRAS G12C mutation.<\/td>\nFirst G12C inhibitor to enter and complete clinical trials. Its binding induces an alternative orientation of His-95, providing a novel surface groove that enhances interaction and improves potency, exhibiting a 10-fold increase in efficacy compared to AR<\/td>\nPreclinical studies showed potential for renal toxicity at high doses and poor brain distribution.<\/td>\n<\/tr>\n
Lonafarnib (SCH66336)<\/strong><\/a><\/td>\nFarnesyltransferase (FTase)<\/td>\n1.9 nM<\/td>\nReduction of mortality risk in Hutchinson-Gilford Progeria Syndrome (HGPS) and treatment of processing-deficient progeroid laminopathies.<\/td>\nFirst approved therapy for reducing mortality risk in HGPS. It is a nonpeptidic, CAAX-competitive, selective FTase inhibitor.<\/td>\nDevelopment for oncology was discontinued due to lack of efficacy, and it has a high incidence of gastrointestinal adverse events.<\/td>\n<\/tr>\n
Adagrasib (MRTX849)<\/strong><\/a><\/td>\nKRAS G12C<\/td>\n5 nM<\/td>\nTreatment of advanced or metastatic solid tumors harboring a KRAS G12C mutation, such as NSCLC and colorectal cancer.<\/td>\nHigh oral bioavailability, long half-life (>50 hours), extensive tissue distribution, and central nervous system penetration. It has >1000-fold selectivity for KRAS G12C over wild-type KRAS.<\/td>\nCommon treatment-related adverse events include nausea, diarrhea, vomiting, fatigue, and increased ALT.<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<\/div>\n
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\"\"KRas \u6291\u5236\u5291<\/span><\/span><\/span><\/span><\/strong><\/span><\/p>\n