{"id":42871,"date":"2023-06-05T18:25:42","date_gmt":"2023-06-05T10:25:42","guid":{"rendered":"https:\/\/biopioneer.com.tw\/?p=42871"},"modified":"2025-11-15T12:59:17","modified_gmt":"2025-11-15T04:59:17","slug":"mrtx-1133-cas2621928-55-8-apexbio%e8%b2%a8%e8%99%9f-b8761","status":"publish","type":"post","link":"https:\/\/biopioneer.com.tw\/?p=42871","title":{"rendered":"MRTX-1133 | CAS#2621928-55-8 APExBIO\u8ca8\u865f B8761"},"content":{"rendered":"

APExBIO\u7cfb\u5217\u5546\u54c1->>MRTX-1133\u00a0<\/span>CAS# 2621928-55-8<\/span><\/span><\/span>
\n<\/span><\/span><\/span><\/strong><\/p>\n

APExBIO Technology LLC \u662f\u4e00\u5bb6\u9818\u5148\u7684\u5c0f\u5206\u5b50\u6291\u5236\u5291 (Small Molecule Inhibitors)\/\u6d3b\u5316\u5291 (Activators)\u3001\u5316\u5408\u7269\u5eab( Compound Libraries)\u3001\u80dc\u80bd(Peptides)\u3001\u6aa2\u6e2c\u8a66\u5291\u76d2(Assay Kits)\u3001\u87a2\u5149\u6a19\u8a18(Fluorescent Label)\u3001\u9176(Enzymes)\u3001\u4fee\u98fe\u6838\u82f7\u9178(Modified Nucleotides)\u3001mRNA \u5408\u6210\u4ee5\u53ca\u5404\u7a2e\u5206\u5b50\u751f\u7269\u5b78\u5de5\u5177\u7684\u4f9b\u61c9\u5546\u3002APExBIO\u63d0\u4f9b\u5ee3\u6cdb\u7684\u7522\u54c1\u7dda\uff0c\u6db5\u84cb 20 \u591a\u500b\u4e0d\u540c\u7684\u7814\u7a76\u9818\u57df\uff0c\u4f8b\u5982\u764c\u75c7(cancer)\u3001\u514d\u75ab\u5b78(immunology)\u3001\u795e\u7d93\u79d1\u5b78(neurosciences)\u3001\u7d30\u80de\u51cb\u4ea1(apoptosis)\u548c\u8868\u89c0\u907a\u50b3\u5b78(epigenetics)\u7b49\u3002\u516c\u53f8\u7e3d\u90e8\u4f4d\u65bc\u7f8e\u570b\u5fb7\u5dde\u4f11\u58eb\u9813USA (Houston, Texas)\uff0c\u81f4\u529b\u65bc\u670d\u52d9\u5168\u7403\u5ba2\u6236\u3002\u9ad8\u5ea6\u91cd\u8996\u7522\u54c1\u54c1\u8cea\u3002\u6240\u6709\u7522\u54c1\u5747\u9075\u5faa\u56b4\u683c\u7684\u751f\u7522\u6307\u5357\uff0c\u4e26\u9644\u6709\u5206\u6790\u8b49\u66f8\u3001HPLC\u3001\u8cea\u8b5c(Mass Spectrum)\u548cHMNR\u4ee5\u53ca\u9ad4\u5916\u9a57\u8b49(in vitro validation)\u3002 APExBIO\u7522\u54c1\u5df2\u88ab\u300aNature\u300b\u3001\u300aCell\u300b\u548c\u300aScience\u300b\u7b49\u773e\u591a\u9802\u7d1a\u540c\u884c\u8a55\u5be9\u671f\u520a\u5f15\u7528\u3002<\/p>\n

<\/p>\n

MRTX-1133 CAS#2621928-55-8 APExBIO\u8ca8\u865f B8761 <\/strong><\/span><\/a><\/span><\/p>\n

selective KRAS G12D inhibitor<\/p>\n

MRTX1133 \u7522\u54c1\u4ecb\u7d39<\/span><\/strong><\/span><\/p>\n

MRTX1133 \u662f\u4e00\u7a2e\u975e\u5171\u50f9(noncovalent)\u7684\u3001\u6709\u6548\u7684\u3001\u9078\u64c7\u6027\u7684 KRAS G12D \u6291\u5236\u5291(selective\u00a0KRAS G12D<\/b> inhibitor)\u3002 MRTX1133 \u6700\u4f73\u5730\u586b\u5145\u4e86\u958b\u95dc II \u53e3\u888b(switch II pocket )\u4e26\u64f4\u5c55\u4e86\u4e09\u500b\u53d6\u4ee3\u57fa\u4ee5\u6709\u5229\u5730\u8207\u86cb\u767d\u8cea\u76f8\u4e92\u4f5c\u7528\uff0c\u5c0e\u81f4\u4f30\u8a08 KD \u5c0d KRAS G12D \u70ba 0.2 pM\u3002 MRTX1133 \u963b\u6b62 SOS1 \u50ac\u5316\u7684\u6838\u82f7\u9178\u4ea4\u63db\u548c\/\u6216 KRAS G12D\/GTP\/RAF1 \u8907\u5408\u7269\u7684\u5f62\u6210\uff0c\u5f9e\u800c\u6291\u5236\u7a81\u8b8a\u7684 KRAS \u4f9d\u8cf4\u6027\u4fe1\u865f\u8f49\u5c0e( mutant KRAS-dependent signal transduction)\u3002MRTX1133 \u6291\u5236 AGS \u7d30\u80de\u7cfb\u4e2d\u7684 ERK \u78f7\u9178\u5316\uff0cIC5\u200b\u200b0 \u7bc4\u570d\u70ba 1-10 nM\uff08AsPC-1\u3001Panc 04.03\u3001Panc 02.03\u3001SW1990\u3001GP2D\u3001Suit2\u3001A427\u3001SNU1033 \u548c HPAC \u7d30\u80de\uff09\u3002\u5728\u4e8c\u7dad\u6d3b\u529b\u6e2c\u5b9a\u4e2d\uff0cMRTX1133 \u5c0d AGS \u7d30\u80de (KRAS G12D) \u7684 IC50 \u70ba 6 nM\uff0c\u540c\u6642\u5c0d MKN1 \u8868\u73fe\u51fa\u8d85\u904e 500 \u500d\u7684\u9078\u64c7\u6027\uff0cMKN1 \u662f\u4e00\u7a2e\u4f9d\u8cf4\u65bc KRAS \u751f\u9577\u548c\u5b58\u6d3b\u7684\u7d30\u80de\u682a\uff0c\u56e0\u70ba\u91ce\u751f\u578b KRAS[1]<\/p>\n

\"COA\u6587\u4ef6_\u5de5\u4f5c\u5340\u57df<\/a><\/p>\n

<\/p>\n\n\n\n\n\n\n\n\n\n\n\n\n
Storage<\/td>\nStore at -20\u00b0C<\/td>\n<\/tr>\n
M.Wt<\/td>\n600.65<\/td>\n<\/tr>\n
Cas No.<\/td>\n2621928-55-8<\/td>\n<\/tr>\n
Formula<\/td>\nC33<\/sub>H31<\/sub>F3<\/sub>N6<\/sub>O2<\/sub><\/td>\n<\/tr>\n
Solubility<\/td>\nSoluble in DMSO<\/td>\n<\/tr>\n
Chemical Name<\/td>\n4-(4-((1R,5S)-3,8-diazabicyclo[3.2.1]octan-3-yl)-8-fluoro-2-(((2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl)methoxy)pyrido[4,3-d]pyrimidin-7-yl)-5-ethynyl-6-fluoronaphthalen-2-ol<\/td>\n<\/tr>\n
SDF<\/td>\nDownload SDF<\/a><\/td>\n<\/tr>\n
Canonical SMILES<\/td>\nC#CC1=C(F)C=CC2=CC(O)=CC(C3=C(F)C4=NC(OC[C@]56C[C@@H](F)CN5CCC6)=NC(N7C[C@H]8N[C@H](CC8)C7)=C4C=N3)=C12<\/td>\n<\/tr>\n
Shipping Condition<\/td>\nSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.<\/td>\n<\/tr>\n
General tips<\/td>\nFor obtaining a higher solubility, please warm the tube at 37\u00b0C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.<\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

 <\/p>\n

\n
\n

APExBIO\u53f0\u7063\u4ee3\u7406\u5546<\/a><\/span><\/strong><\/p>\n<\/div>\n<\/div>\n

https:\/\/www.apexbt.com<\/a><\/span><\/p>\n

APExBIO\u63d0\u4f9b\u512a\u8cea\u7684\u80dc\u80bd\u548c\u751f\u7269\u5206\u6790\u8a66\u5291\uff0c\u5ee3\u6cdb\u7522\u54c1\u7dda\u5982Protease\u3001Chromatin\/Epigenetics\u8868\u89c0\u907a\u50b3\u5b78\u3001MAPK Signal\u3001DNA Damege\/DNA repair\u3001\u7d30\u80de\u51cb\u4ea1\u3001\u816b\u7624\u751f\u7269\u5b78\u3001Stem cell\u7b49\u7814\u7a76\u9818\u57df\uff0c \u9084\u63d0\u4f9b\u5b9a\u5236\u7684\u670d\u52d9\uff0c\u5305\u62ec\u591a\u80bd\u5408\u6210\uff0c\u6297\u9ad4\u7684\u751f\u7522\u548c\u6aa2\u6e2c\u7684\u767c\u5c55\u3002\u7522\u54c1\u7ddaDNA\/RNA prep kit\u3001Drug Screening panel\u3001Bioactive peptides\u3001Growth factors\u3001Biotinylation Reagents\u3001tag peptides\u3001amino Acids\u3001Growth factors\u7b49\u3002APExBIO\u7522\u54c1\u8cea\u91cf\u90fd\u4f34\u96a8\u8457\u8b49\u66f8\u7684\u5206\u6790\uff0c\u9ad8\u6548\u6db2\u76f8\u8272\u8b5c\uff0c\u8cea\u8b5c\uff0c\u548cHMNR\u6578\u64da\u3002<\/p>\n

\"\u578b\u9304\u4e0b\u8f09\"<\/a><\/p>\n

<\/p>\n","protected":false},"excerpt":{"rendered":"

APExBIO\u7cfb\u5217\u5546\u54c1->>MRTX-1133\u00a0CAS# 2621928-55-8 APExBIO […]<\/p>\n","protected":false},"author":3,"featured_media":47343,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":[],"categories":[5368],"tags":[5786],"_links":{"self":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/42871"}],"collection":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts"}],"about":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/types\/post"}],"author":[{"embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/users\/3"}],"replies":[{"embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fcomments&post=42871"}],"version-history":[{"count":7,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/42871\/revisions"}],"predecessor-version":[{"id":53609,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/42871\/revisions\/53609"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/media\/47343"}],"wp:attachment":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=42871"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=42871"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=42871"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}