{"id":42765,"date":"2023-05-30T16:01:35","date_gmt":"2023-05-30T08:01:35","guid":{"rendered":"https:\/\/biopioneer.com.tw\/?p=42765"},"modified":"2025-09-02T15:32:12","modified_gmt":"2025-09-02T07:32:12","slug":"ruxolitinib-cas-941678-49-5-mce%e8%b2%a8%e8%99%9fhy-50856","status":"publish","type":"post","link":"https:\/\/biopioneer.com.tw\/?p=42765","title":{"rendered":"Ruxolitinib | CAS# 941678-49-5\u00a0 MCE\u8ca8\u865fHY-50856\u00a0"},"content":{"rendered":"

MCE (MedChem Express)<\/span> -Ruxolitinib (INCB18424) potent and selective JAK1\/2 inhibitor \u00a0<\/span><\/span><\/span><\/strong><\/span><\/p>\n

MCE\u7e3d\u90e8\u4f4d\u65bc\u7f8e\u570b\u65b0\u6fa4\u897f\uff0c\u63d0\u4f9b\u7a2e\u985e\u9f4a\u5168\u7684\u5316\u5b78\u53ca\u751f\u5316\u7814\u7a76\u7528\u7522\u54c1\uff0c\u5305\u62ec\u5275\u65b0\u7684\u751f\u547d\u79d1\u5b78\u8a66\u5291\uff0creference compounds(\u6a19\u6e96\u5316\u5408\u7269)\uff0cAPIs(\u539f\u6599\u85e5)\u53caNatural compounds(\u5929\u7136\u5316\u5408\u7269)\u4ee5\u63d0\u4f9b\u5be6\u9a57\u5ba4\u6216\u79d1\u5b78\u7814\u7a76\u4e4b\u7528\uff0cMedChemExpress(MCE)\u7522\u54c150000+ \u7279\u7570\u6027\u6291\u5236\u5291\u3001\u5316\u5408\u7269\u5eab\u3001\u91cd\u7d44\u86cb\u767d\uff0c\u5c08\u6ce8\u65bc\u4fe1\u865f\u901a\u8def\u548c\u75be\u75c5\u7814\u7a76\u9818\u57df\u3002\u5168\u7403\u6587\u737b\u5ee3\u6cdb\u5f15\u7528\uff0c\u8cea\u63a7\u9ad4\u7cfb\u56b4\u683c\uff0c\u54c1\u8cea100%\u3002<\/p>\n

<\/p>\n

Ruxolitinib| CAS# 941678-49-5\u00a0 MCE\u8ca8\u865fHY-50856\u00a0<\/span><\/strong><\/span><\/a><\/p>\n

Ruxolitinib (INCB18424) \u662f\u4e00\u7a2e\u6709\u6548\u7684\u9078\u64c7\u6027 JAK1\/2 \u6291\u5236\u5291\uff0c\u7121\u7d30\u80de\u8a66\u9a57(cell-free assays)\u4e2d\u7684 IC50 \u5206\u5225\u70ba 3.3 nM \u548c 2.8 nM\uff0c\u5c0d JAK1\/2 \u7684\u9078\u64c7\u6027\u662f\u5c0d JAK3 \u7684 130 \u500d\u3002 Ruxolitinib \u8a98\u5c0e\u81ea\u566c(autophagy )\u4e26\u901a\u904e\u6bd2\u6027\u7dda\u7c92\u9ad4(toxic mitophagy)\u81ea\u566c\u6bba\u6b7b\u816b\u7624\u7d30\u80de(kills tumor cells)\u3002Ruxolitinib (INCB18424) is a potent and selective JAK1\/2 inhibitor with IC50s of 3.3 nM and 2.8 nM in cell-free assays, and has 130-fold selectivity for JAK1\/2 over JAK3. Ruxolitinib induces autophagy and kills tumor cells through toxic mitophagy.<\/p>\n

<\/p>\n

Ruxolitinib \u6709\u6548\u4e14\u9078\u64c7\u6027\u5730\u6291\u5236 JAK2V617F \u4ecb\u5c0e\u7684\u4fe1\u865f\u50b3\u5c0e(signaling)\u548c\u589e\u6b96(proliferation)\uff0c\u4ee5\u5291\u91cf\u4f9d\u8cf4\u6027\u65b9\u5f0f(dose dependent manner)\u986f\u8457\u589e\u52a0\u7d30\u80de\u51cb\u4ea1(apoptosis)\uff0c\u4e26\u4e14\u5728 64 nM \u6642\u5c0e\u81f4 Ba\/F3 \u7d30\u80de\u4e2d\u5177\u6709\u53bb\u6975\u5316\u7dda\u7c92\u9ad4(depolarized mitochondria)\u7684\u7d30\u80de\u52a0\u500d\u3002Ruxolitinib \u5c0d\u7d05\u7d30\u80de\u96c6\u843d\u5f62\u6210(erythroid colony formation)\u5177\u6709\u986f\u8457\u7684\u6548\u529b\uff0cIC50 \u70ba 67 nM\uff0c\u4e26\u6291\u5236\u4f86\u81ea\u6b63\u5e38\u4f9b\u9ad4\u548c\u771f\u6027\u7d05\u7d30\u80de\u589e\u591a\u75c7\u60a3\u8005\u7684\u7d05\u7d30\u80de\u7956\u7d30\u80de(erythroid progenitors)\u589e\u6b96\uff0cIC50 \u503c\u5206\u5225\u70ba 407 nM \u548c 223 nM[1]\u3002
\nRuxolitinib\uff08180 mg\/kg\uff0c\u53e3\u670d\uff0c\u6bcf\u5929\u5169\u6b21\uff09\u5c0e\u81f4\u7b2c 22 \u5929\u6642\u7684\u5b58\u6d3b\u7387\u8d85\u904e 90%\uff0c\u4e26\u986f\u8457\u964d\u4f4e\u813e\u816b\u5927\u548c\u708e\u75c7\u7d30\u80de\u56e0\u5b50\u7684\u5faa\u74b0\u6c34\u5e73\uff0c\u4e26\u512a\u5148\u6d88\u9664\u816b\u7624\u7d30\u80de\uff0c\u5f9e\u800c\u986f\u8457\u5ef6\u9577\u5b58\u6d3b\u6642\u9593\uff0c\u800c\u7121\u9aa8\u9ad3\u6291\u88fd\u6216JAK2V617F \u9a45\u52d5\u7684\u5c0f\u9f20\u6a21\u578b\u4e2d\u7684\u514d\u75ab\u6291\u88fd\u4f5c\u7528 [1]\u3002\u5728 Ruxolitinib \u7d44\u4e2d\uff0c41.9% \u7684\u60a3\u8005\u9054\u5230\u4e86\u4e3b\u8981\u7d42\u9ede\uff0c\u800c\u5728\u9aa8\u9ad3\u7e96\u7dad\u5316\u7684\u96d9\u76f2\u8a66\u9a57\u4e2d\uff0c\u5b89\u6170\u5291\u7d44\u7684\u9019\u4e00\u6bd4\u4f8b\u70ba 0.7%\u3002 Ruxolitinib \u5c0e\u81f4\u813e\u81df\u9ad4\u7a4d\u6e1b\u5c11\u548c\u7e3d\u75c7\u72c0\u8a55\u5206\u6539\u5584 50% \u6216\u66f4\u591a[2]\u3002<\/p>\n

<\/p>\n

<\/p>\n

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\"\u7db2\u7ad9\u898f\u683c\u5c0f\u5716_\u5de5\u4f5c\u5340\u57df<\/a><\/p>\n

<\/p>\n

CAS No. :\u00a0941678-49-5<\/a><\/p>\n

\"\"<\/p>\n

MedChemexpress (MCE) \u7522\u54c1\u985e\u5225\uff0d\u4f9d\u7814\u7a76\u985e\u578b\u5340\u5206\uff1a<\/span><\/h4>\n

\u2022Anti-infection<\/a><\/span><\/strong><\/h4>\n

\u2022Antibody-drug Conjugate\/ADC Related<\/a><\/span><\/strong><\/h4>\n

\u2022Apoptosis<\/a><\/span><\/strong><\/h4>\n

\u2022Autophagy<\/a><\/span><\/strong><\/h4>\n

\u2022Cell Cycle\/DNA Damage<\/a><\/span><\/strong><\/h4>\n

\u2022Cytoskeleton<\/a><\/span><\/strong><\/h4>\n

\u2022Epigenetics<\/a><\/span><\/strong><\/h4>\n

\u2022GPCR\/G Protein<\/a><\/span><\/strong><\/h4>\n

\u2022Immunology\/Inflammation<\/a><\/span><\/strong><\/h4>\n

\u2022JAK\/STAT Signaling<\/a>\u2022MAPK\/ERK Pathway<\/a><\/span><\/strong><\/h4>\n

\u2022Membrane Transporter\/Ion Channel<\/a><\/span><\/strong><\/h4>\n

\u2022Metabolic Enzyme\/Protease<\/a><\/span><\/strong><\/h4>\n

\u2022Neuronal Signaling<\/a><\/span><\/strong><\/h4>\n

\u2022NF-\u03baB<\/a><\/span><\/strong><\/h4>\n

\u2022PI3K\/Akt\/mTOR<\/a><\/span><\/strong><\/h4>\n

\u2022PROTAC<\/a><\/span><\/strong><\/h4>\n

\u2022Protein Tyrosine Kinase\/RTK<\/a>\u2022Stem Cell\/Wnt<\/a><\/span><\/strong><\/h4>\n

\u2022TGF-beta\/Smad<\/a><\/span><\/strong><\/h4>\n

\u2022Vitamin D Related<\/a><\/span><\/strong><\/h4>\n

\u2022Others<\/a><\/span><\/strong><\/h4>\n","protected":false},"excerpt":{"rendered":"

MCE (MedChem Express) -Ruxolitinib (INCB18424) potent a […]<\/p>\n","protected":false},"author":3,"featured_media":52829,"comment_status":"closed","ping_status":"closed","sticky":false,"template":"","format":"standard","meta":[],"categories":[5369],"tags":[6867,5784,6866,6869,6865,6868],"_links":{"self":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/42765"}],"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=42765"}],"version-history":[{"count":7,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/42765\/revisions"}],"predecessor-version":[{"id":52831,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/posts\/42765\/revisions\/52831"}],"wp:featuredmedia":[{"embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=\/wp\/v2\/media\/52829"}],"wp:attachment":[{"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fmedia&parent=42765"}],"wp:term":[{"taxonomy":"category","embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Fcategories&post=42765"},{"taxonomy":"post_tag","embeddable":true,"href":"https:\/\/biopioneer.com.tw\/index.php?rest_route=%2Fwp%2Fv2%2Ftags&post=42765"}],"curies":[{"name":"wp","href":"https:\/\/api.w.org\/{rel}","templated":true}]}}