{"id":54962,"date":"2026-08-04T14:06:15","date_gmt":"2026-08-04T06:06:15","guid":{"rendered":"https:\/\/biopioneer.com.tw\/?p=54962"},"modified":"2026-08-04T14:40:47","modified_gmt":"2026-08-04T06:40:47","slug":"kras-g12c-%e6%8a%91%e5%88%b6%e5%8a%91-daraxonrasib-rmc-6236-cas-2765081-21-6-selleck%e8%b2%a8%e8%99%9f-e1597","status":"publish","type":"post","link":"https:\/\/biopioneer.com.tw\/?p=54962","title":{"rendered":"KRAS-G12C \u6291\u5236\u5291-Daraxonrasib (RMC-6236)\u00a0 | CAS# 2765081-21-6 Selleck\u8ca8\u865f E1597"},"content":{"rendered":"
\n

Selleck chemicals \u7cfb\u5217\u5546\u54c1->><\/span><\/span><\/span><\/span><\/strong>KRas \u6291\u5236\u5291\/Daraxonrasib (RMC-6236)<\/span><\/span><\/span><\/span><\/p>\n

Daraxonrasib (RMC-6236) \u662f\u4e00\u7a2eRAS(ON)\u591a\u9078\u64c7\u6027\u975e\u5171\u50f9\u6291\u5236\u5291\uff0c\u53ef\u6291\u5236\u7d93\u5178 RAS \u4e9e\u578b\u7a81\u8b8a\u9ad4\u548c\u91ce\u751f\u578b\u7684\u6d3b\u6027 GTP \u7d50\u5408\u72c0\u614b\uff0c\u5177\u6709\u5ee3\u6cdb\u7684\u6cbb\u7642\u6f5b\u529b\u3002 RMC-6236 \u5728 RAS \u4f9d\u8cf4\u6027\u7d30\u80de\u682a\u4e2d\u8868\u73fe\u51fa\u5f37\u5927\u7684\u6297\u764c\u529f\u6548\uff0c\u5c24\u5176\u5c0d KRAS 12 \u865f\u5bc6\u78bc\u5b50\u7a81\u8b8a\u7684\u7d30\u80de\u682a\u6548\u679c\u986f\u8457\u3002<\/p>\n

KRAS-G12C \u6291\u5236\u5291-Daraxonrasib (RMC-6236)\u00a0 | CAS# 2765081-21-6 Selleck\u8ca8\u865f E1597<\/a><\/span><\/p>\n

Daraxonrasib is a potent pan-KRAS inhibitor. It affects RAS signaling by targeting RAS(ON), inhibiting cell viability.<\/p>\n

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

<\/p>\n

Daraxonrasib (RMC-6236) \u662f\u4e00\u7a2eRAS(ON)\u591a\u9078\u64c7\u6027\u975e\u5171\u50f9\u6291\u5236\u5291\uff0c\u53ef\u6291\u5236\u7d93\u5178 RAS \u4e9e\u578b\u7a81\u8b8a\u9ad4\u548c\u91ce\u751f\u578b\u7684\u6d3b\u6027 GTP \u7d50\u5408\u72c0\u614b\uff0c\u5177\u6709\u5ee3\u6cdb\u7684\u6cbb\u7642\u6f5b\u529b\u3002 RMC-6236 \u5728 RAS \u4f9d\u8cf4\u6027\u7d30\u80de\u682a\u4e2d\u8868\u73fe\u51fa\u5f37\u5927\u7684\u6297\u764c\u529f\u6548\uff0c\u5c24\u5176\u5c0d KRAS 12 \u865f\u5bc6\u78bc\u5b50\u7a81\u8b8a\u7684\u7d30\u80de\u682a\u6548\u679c\u986f\u8457\u3002\u80f0\u817a\u5c0e\u7ba1\u817a\u764c (PDAC)Daraxonrasib (RMC-6236) \u5728\u651c\u5e36 RAS \u7a81\u8b8a\u4e14\u5148\u524d\u63a5\u53d7\u904e\u6cbb\u7642\u7684\u8f49\u79fb\u6027\u80f0\u817a\u5c0e\u7ba1\u817a\u764c\u60a3\u8005\u4e2d\uff0c\u5c55\u73fe\u51fa\u4e86\u524d\u6240\u672a\u6709\u7684\u7e3d\u751f\u5b58\u671f (OS) \u548c\u7121\u9032\u5c55\u751f\u5b58\u671f (PFS) \u7372\u76ca\u3002\u5305\u62ec RASolute 302 \u5728\u5167\u7684\u8fd1\u671f 3 \u671f\u81e8\u5e8a\u8a66\u9a57\u8868\u660e\uff0c\u8a72\u85e5\u7269\u986f\u8457\u512a\u65bc\u6a19\u6e96\u7684\u7d30\u80de\u6bd2\u6027\u5316\u7642\u3002\u4f5c\u70ba\u9996\u6b3e\u540c\u985e\uff08first-in-class\uff09\u53e3\u670d RAS(ON) \u591a\u91cd\u9078\u64c7\u6027\u6291\u5236\u5291\uff0c\u5b83\u80fd\u6709\u6548\u9776\u5411\u7a81\u8b8a\u578b\u53ca\u91ce\u751f\u578b RAS \u86cb\u767d\u3002\u9019\u9805\u7a81\u7834\u6027\u9032\u5c55\u89e3\u6c7a\u4e86\u91dd\u5c0d\u9019\u7a2e\u9ad8\u81f4\u6b7b\u6027\u60e1\u6027\u816b\u7624\u7684\u4e00\u9805\u95dc\u9375\u672a\u6eff\u8db3\u91ab\u7642\u9700\u6c42\uff0c\u5f9e\u800c\u5f15\u767c\u4e86\u5ee3\u6cdb\u7684\u79d1\u5b78\u95dc\u6ce8\uff0c\u4e26\u6709\u671b\u5728\u5168\u7403\u7bc4\u570d\u5167\u7372\u5f97\u5feb\u901f\u76e3\u7ba1\u6279\u51c6\u3002\u5728\u975e\u5c0f\u7d30\u80de\u80ba\u764c (NSCLC)\u4e2d\uff0cDaraxonrasib \u7684\u7814\u7a76\u4e3b\u8981\u96c6\u4e2d\u5728\u651c\u5e36\u7279\u5b9a RAS \u7a81\u8b8a\u4e14\u5148\u524d\u63a5\u53d7\u904e\u6a19\u6e96\u6cbb\u7642\u5f8c\u75c5\u60c5\u9032\u5c55\u7684\u975e\u5c0f\u7d30\u80de\u80ba\u764c\u60a3\u8005\u3002\u5305\u62ec RASolve 301 \u7814\u7a76\u5728\u5167\u7684\u5168\u7403 III \u671f\u81e8\u5e8a\u8a66\u9a57\u6b63\u5728\u7a4d\u6975\u8a55\u4f30\u5176\u7642\u6548\u3001\u5b89\u5168\u6027\u548c\u85e5\u7269\u52d5\u529b\u5b78\uff0c\u4e26\u8207\u591a\u897f\u4ed6\u8cfd\u7b49\u6a19\u6e96\u7642\u6cd5\u9032\u884c\u6bd4\u8f03\u3002\u4f5c\u70ba\u4e00\u7a2e\u5f37\u6548\u7684\u6cdb RAS \u5206\u5b50\u81a0\u6291\u5236\u5291\uff0cDaraxonrasib \u65e8\u5728\u900f\u904e\u5ee3\u6cdb\u9776\u5411 RAS \u540c\u5de5\u9176\u7684\u6d3b\u6027\u72c0\u614b\u4f86\u514b\u670d\u73fe\u6709\u7a81\u8b8a\u7279\u7570\u6027\u6291\u5236\u5291\u7684\u5c40\u9650\u6027\uff0c\u5f9e\u800c\u70ba\u9019\u7a2e\u5e38\u898b\u4e14\u68d8\u624b\u7684\u764c\u75c7\u985e\u578b\u63d0\u4f9b\u4e00\u7a2e\u5099\u53d7\u671f\u5f85\u7684\u9776\u5411\u6cbb\u7642\u9078\u64c7\u3002\u5927\u8178\u76f4\u8178\u764c (CRC) \u9054\u62c9\u897f\u5e03 (Daraxonrasib) \u6b63\u88ab\u5ee3\u6cdb\u7814\u7a76\uff0c\u4f5c\u70ba\u4e00\u7a2e\u6709\u524d\u666f\u7684\u6a19\u9776\u6cbb\u7642\u624b\u6bb5\uff0c\u7528\u65bc\u6cbb\u7642\u651c\u5e36\u591a\u7a2e\u81f4\u764c RAS \u7a81\u8b8a\u7684\u8f49\u79fb\u6027\u6216\u4e0d\u53ef\u5207\u9664\u7684\u7d50\u76f4\u8178\u764c\u3002\u76ee\u524d\u6b63\u5728\u9032\u884c\u7684\u65e9\u671f\u81e8\u5e8a\u8a66\u9a57\u548c\u806f\u5408\u81e8\u5e8a\u8a66\u9a57\u6b63\u5728\u56b4\u683c\u8a55\u4f30\u5176\u5b89\u5168\u6027\u3001\u8010\u53d7\u6027\u548c\u521d\u6b65\u6297\u816b\u7624\u6d3b\u6027\u3002\u7531\u65bc RAS \u7a81\u8b8a\u5728\u7d50\u76f4\u8178\u764c\u4e2d\u666e\u904d\u5b58\u5728\uff0c\u4e26\u4e14\u901a\u5e38\u6703\u5c0e\u81f4\u5c0d\u50b3\u7d71\u6a19\u9776\u7642\u6cd5\u7684\u6297\u85e5\u6027\uff0c\u9019\u7a2e\u65b0\u578b\u591a\u9078\u64c7\u6027 RAS(ON) \u6291\u5236\u5291\u63d0\u4f9b\u4e86\u4e00\u7a2e\u91cd\u8981\u7684\u5168\u65b0\u6cbb\u7642\u7b56\u7565\u3002\u7814\u7a76\u4eba\u54e1\u5c24\u5176\u95dc\u6ce8\u5176\u8a98\u5c0e\u6df1\u5ea6\u5206\u5b50\u53cd\u61c9\u7684\u6f5b\u529b\uff0c\u4ee5\u53ca\u5176\u8207\u80c3\u8178\u9053\u60e1\u6027\u816b\u7624\u4e2d\u7684\u5176\u4ed6\u6297\u816b\u7624\u85e5\u7269\u806f\u5408\u4f7f\u7528\u6642\u7684\u5354\u540c\u6548\u61c9\u3002<\/p>\n<\/div>\n

\n
\n
\n\n\n\n\n\n\n\n\n
Storage<\/td>\n
M.Wt<\/td>\n811.05<\/td>\n<\/tr>\n
Cas No.<\/td>\n2765081-21-6<\/td>\n<\/tr>\n
Formula<\/td>\nC44<\/sub>H58<\/sub>N8<\/sub>O5<\/sub>S<\/td>\n<\/tr>\n
Synonyms<\/td>\nRMC-6236; RAS-IN-2<\/td>\n<\/tr>\n
Solubility<\/td>\nDMSO : 100 mg\/mL (123.29 mM)
\n(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)Ethanol : 100 mg\/mLWater : Insoluble<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n<\/div>\n<\/div>\n
<\/div>\n
<\/div>\n
\"\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
\n

\"\"KRas \u6291\u5236\u5291<\/span><\/span><\/span><\/span><\/strong><\/span><\/p>\n