{"id":35431,"date":"2022-10-26T15:38:53","date_gmt":"2022-10-26T07:38:53","guid":{"rendered":"http:\/\/biopioneer.com.tw\/?p=35431"},"modified":"2025-11-15T15:55:01","modified_gmt":"2025-11-15T07:55:01","slug":"s-crizotinib-cas877399-52-51374356-45-2-apexbio-%e8%b2%a8%e8%99%9fa8802","status":"publish","type":"post","link":"https:\/\/biopioneer.com.tw\/?p=35431","title":{"rendered":"(S)-Crizotinib | CAS#877399-52-5;1374356-45-2 APExBIO \u8ca8\u865fA8802"},"content":{"rendered":"

\u81ea\u566c\u7cfb\u5217\u5546\u54c1->>(S)-Crizotinib<\/span><\/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>>\u66f4\u591aAPExBio\u5546\u54c1<\/span><\/strong><\/em><\/span><\/a><\/p>\n

<\/p>\n

(S)-Crizotinib | CAS#877399-52-5;1374356-45-2 APExBIO\u00a0 \u8ca8\u865fA8802<\/a><\/span><\/p>\n

Potent MTH1 inhibitor<\/p>\n

(S)-crizotinib \u9078\u64c7\u6027\u6291\u5236 MTH1 \u50ac\u5316\u6d3b\u6027\uff0cIC50 \u70ba 72 nM\uff0c\u800c\u81e8\u5e8a\u4f7f\u7528\u7684 (R)-\u5c0d\u6620\u7570\u69cb\u9ad4\u7121\u6d3b\u6027\uff0cIC50 \u70ba 1375 nM\u3002\u6b64\u5916\uff0c\u8207 (R)-\u5c0d\u6620\u7570\u69cb\u9ad4\u76f8\u6bd4\uff0c\u76f4\u63a5\u7d50\u5408\u6e2c\u5b9a (ITC) \u8868\u660e (S)-\u5c0d\u6620\u7570\u69cb\u9ad4\u5c0d MTH1 \u7684\u89aa\u548c\u529b\u9ad8 16 \u500d\u3002\u901a\u904e\u4f7f\u7528 Km \u6fc3\u5ea6\u7684\u5e95\u7269\uff0c(S)-crizotinib \u548c MTH1 \u5e95\u7269 8-oxo-dGTP \u548c 2-OH-dATP \u7684\u5e73\u5747 IC50 \u503c\u5206\u5225\u70ba 330 nM \u548c 408 nM\u3002 (S)-crizotinib \u6709\u6548\u6291\u5236 SW480 \u7d30\u80de\u548c KRAS \u7a81\u8b8a\u7684 PANC1 \u7d30\u80de\u7684\u96c6\u843d\u5f62\u6210\uff0c\u985e\u4f3c\u65bc SCH51344\u3002\u6b64\u5916\uff0c\u9ad4\u5916 Kd \u6e2c\u91cf\u8868\u660e\uff0c(S)-\u514b\u5511\u66ff\u5c3c\u5c0d\u65e2\u5b9a\u9776\u6a19 ALK\u3001MET \u548c ROS1 \u7684\u6548\u529b\u9060\u4f4e\u65bc (R)-\u5c0d\u6620\u7570\u69cb\u9ad4\u3002 (S)-crizotinib \u672a\u6aa2\u6e2c\u5230\u5c0d SW480 \u7d30\u80de\u589e\u6b96\u7684\u4efb\u4f55\u986f\u8457\u5f71\u97ff\uff0c\u4e26\u4e14\u5c0d SV40T \u548c KRASV12 \u7d30\u80de\u5177\u6709\u6700\u9ad8\u7684\u6bd2\u6027\u3002 (S)-crizotinib \u8207 (R)-crizotinib \u76f8\u6bd4\uff0c\u6709\u6548\u5730\u7a69\u5b9a\u4e86 MTH1\uff0c\u4f7f\u7528\u7d30\u80de\u71b1\u4f4d\u79fb\u6e2c\u5b9a\u9a57\u8b49\u4e86 BJ-KRASV12 \u7d30\u80de\u5167\u7684\u5dee\u7570\u9776\u5411\u3002 (S)-crizotinib \u8a98\u5c0e DNA \u55ae\u93c8\u65b7\u88c2\u589e\u52a0\uff0c\u6fc0\u6d3b\u4eba\u7d50\u8178\u764c\u7d30\u80de(human colon carcinoma cells)\u4e2d\u7684 DNA \u4fee\u5fa9(DNA repair)\uff0c\u4e26\u6709\u6548\u6291\u5236\u52d5\u7269\u6a21\u578b\u4e2d\u7684\u816b\u7624\u751f\u9577(tumour growth)\uff0c\u9019\u662f\u901a\u904e MTH1 \u6291\u5236\u7834\u58de\u6838\u82f7\u9178\u6c60\u7a69\u614b(nucleotide pool homeostasis)\u7684\u7d50\u679c\u3002\u9ad4\u5167\u5c0f\u9f20\u7570\u7a2e\u79fb\u690d\u7814\u7a76\u8868\u660e\uff0c(S)-\u514b\u5511\u66ff\u5c3c\uff0c\u800c\u4e0d\u662f (R)-\u5c0d\u6620\u7570\u69cb\u9ad4\uff0c\u80fd\u5920\u640d\u5bb3\u6574\u9ad4\u816b\u7624\u9032\u5c55\uff0c\u4e26\u7279\u5225\u6e1b\u5c11\u816b\u7624\u9ad4\u7a4d\u8d85\u904e 50%\u3002<\/p>\n

\"\"<\/p>\n

\"\"<\/p>\n\n\n\n\n\n\n\n\n\n\n\n\n\n
Physical Appearance<\/td>\nA solid<\/td>\n<\/tr>\n
Storage<\/td>\nStore at -20\u00b0C<\/td>\n<\/tr>\n
M.Wt<\/td>\n450.34<\/td>\n<\/tr>\n
Cas No.<\/td>\n877399-52-5;1374356-45-2<\/td>\n<\/tr>\n
Formula<\/td>\nC21H22Cl2FN5O<\/td>\n<\/tr>\n
Solubility<\/td>\n\u226533.33 mg\/mL in DMSO; insoluble in H2O; \u22658.58 mg\/mL in EtOH with ultrasonic<\/td>\n<\/tr>\n
Chemical Name<\/td>\n3-[(1S)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-5-(1-piperidin-4-ylpyrazol-4-yl)pyridin-2-amine<\/td>\n<\/tr>\n
SDF<\/td>\nDownload SDF<\/a><\/td>\n<\/tr>\n
Canonical SMILES<\/td>\nCC(C1=C(C=CC(=C1Cl)F)Cl)OC2=C(N=CC(=C2)C3=CN(N=C3)C4CCNCC4)N<\/td>\n<\/tr>\n
Shipping Condition<\/td>\nShip with blue ice, or upon other requests.<\/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

\"\"<\/strong><\/p>\n

<\/p>\n

APExBIO\u53f0\u7063\u4ee3\u7406\u5546:\u00a0 <\/span><\/strong><\/span><\/a>https:\/\/www.apexbt.com\/<\/span><\/span><\/a><\/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
\n\"\u578b\u9304\u4e0b\u8f09\"<\/a><\/p>\n\n\n\n\n\n\n\n\n\n\n\n
DNA Damage\/DNA Repair<\/strong><\/span><\/td>\nCAS#<\/span><\/td>\n#\u8ca8\u865f<\/span><\/td>\n\u61c9\u7528<\/span><\/td>\n<\/tr>\n
SCR7<\/a><\/span><\/td>\nCAS#1533426-72-0<\/span><\/td>\n\u8ca8\u865fA8705<\/span><\/td>\nDNA ligase IV inhibitor<\/span><\/td>\n<\/tr>\n
RHPS4n\u00a0<\/a>\u00a0<\/span><\/td>\nCAS#390362-78-4<\/span><\/td>\n\u8ca8\u865fB6186<\/span><\/td>\nTelomerase inhibitor<\/span><\/td>\n<\/tr>\n
AZD6738<\/a><\/span><\/td>\nCAS#1352226-88-0<\/span><\/td>\n\u8ca8\u865fB6007<\/span><\/td>\nATR inhibitor<\/span><\/td>\n<\/tr>\n
\n

ORY-1001<\/a><\/span><\/p>\n

 <\/td>\n

CAS#1431326-61-2<\/span><\/td>\n\u8ca8\u865fB5882<\/span><\/td>\nSelective inhibitor of KDM1A.<\/span><\/td>\n<\/tr>\n
RGFP966<\/a><\/span><\/td>\nCAS#1357389-11-7;1396841-57-8<\/span><\/td>\n\u8ca8\u865fA8803<\/span><\/td>\nSpecific HDAC3 inhibitor<\/span><\/td>\n<\/tr>\n
Oxaliplatin<\/a><\/span><\/td>\nCAS#61825-94-3<\/span><\/td>\n\u8ca8\u865fA8648<\/span><\/td>\nAntitumor agent<\/span><\/td>\n<\/tr>\n
(S)-Crizotinib<\/a><\/span><\/td>\nCAS#877399-52-5;1374356-45-2<\/span><\/td>\n\n

\u8ca8\u865fA8802<\/span><\/p>\n

 <\/td>\n

Potent MTH1 inhibitor<\/span><\/td>\n<\/tr>\n
Tubastatin A<\/a><\/span><\/td>\nCAS#1252003-15-8<\/span><\/td>\n\u8ca8\u865fA4101<\/span><\/td>\nHDAC6 inhibitor,potent and selective<\/span><\/td>\n<\/tr>\n<\/tbody>\n<\/table>\n

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

\u81ea\u566c\u7cfb\u5217\u5546\u54c1->>(S)-Crizotinib APExBIO Technology LLC \u662f\u4e00 […]<\/p>\n","protected":false},"author":3,"featured_media":34308,"comment_status":"open","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":[],"categories":[5368,3],"tags":[5026],"_links":{"self":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/35431"}],"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=35431"}],"version-history":[{"count":5,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/35431\/revisions"}],"predecessor-version":[{"id":53767,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/35431\/revisions\/53767"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/media\/34308"}],"wp:attachment":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=35431"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=35431"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=35431"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}