阿拉丁小分子抑制劑、激動劑、拮抗劑--JAK/STAT信號通路

來源: 上海阿拉丁生化科技股份有限公司   2019-12-9   訪問量:938評論(0)

parent;">T162509酪氨酸激酶抑制劑 AG 494>98.0%(HPLC)(N)133550-35-320mg,100mgEGFR1.2 μMEGF6 μMC125447Canertinib (CI-1033)≥98%267243-28-710mg,50mg,250mgEGFR1.5 nMErbB29.0 nML126696Lapatinib≥99%231277-92-225mg,100mg,250mg,500mg,1g,5g無細胞EGFR10.2 nMErbB29.8 nMA126525AG-490 (Tyrphostin B42)≥98%133550-30-820mg,50mg,250mg,1g無細胞EGFR0.1 μMC129397CP-724714≥99%537705-08-15mg,10mg,25mg,50mg HER2/ErbB210 nMD129347Dacomitinib (PF299804, PF299)≥99%1110813-31-45mg,10mg,50mg,250mg無細胞EGFR6 nMW127713WZ4002≥98%1213269-23-810mg,50mg,100mgBaF3細胞系EGFR(L858R)2 nMEGFR(T790M)8 nMA129380AZD8931 (Sapitinib)≥98%848942-61-05mg,10mg,50mgEGFR4 nMErbB23 nMErbB34 nMC127191CUDC-101≥98%1012054-59-910mg,25mg,50mg,100mg,250mgHDAC4.4 nMEGFR2.4 nMHER215.7 nMA126582AG-1478 (Tyrphostin AG-1478)≥98%153436-53-45mg,10mg,25mg,50mg無細胞EGFR3 nMP129384PD153035 HCl≥98%(HPLC)183322-45-410mg,50mg,250mg EGFR29 pM5.2 pMP125444Pelitinib≥98%257933-82-75mg,25mg,100mg EGFR38.5 nMB126145AC480 (BMS-599626)≥98%714971-09-25mg,25mg,100mgHER120 nMHER230 nMA126830AEE788 (NVP-AEE788)≥97%497839-62-05mg,25mg,100mgEGFR2 nMHER2/ErbB26 nMA127691AP26113≥98%1197958-12-55mg,10mg,25mg,50mg,100mgALKEGFRO125033OSI-420≥99%183320-51-65mg,10mg,50mg EGFR2 nMW127717WZ3146≥98%1214265-56-15mg,25mg,100mgEGFR(L858R)2 nMEGFR(E746_A750)2 nMA126334ARRY-380≥98%937265-83-35mg,10mg,50mg HER28 nMW126471WZ8040≥98%1214265-57-25mg,25mg,50mg EGFRT790MA129426AST-1306 TsOH≥98%1050500-29-25mg,10mg,50mgEGFR0.5 nMErbB23 nMC124905CO-1686 (AVL-301)≥99%1374640-70-65mg,10mg,50mg,100mg無細胞EGFRL858R/T790M21.5 nMEGFRWT303.3 nMG106672金雀異黃酮分析標準品,≥98%446-72-020mg,1g,5gNIH-3T3細胞EGF12μM胰島素19 μMG106673金雀異黃酮97%446-72-0100mg,500mg,1g,5g,25gNIH-3T3細胞EGF12μM胰島素19 μMV129433Varlitinib≥96%845272-21-15mg,10mg,50mgErbB1(EGFR)7 nMErbB2(HER2)2 nMI129405Icotinib≥99%610798-31-75mg,10mg,50mg EGFR5 nMT126234TAK-285≥98%871026-44-75mg,10mg,50mgHER2和EGFR(HER1)17 nMHER2和EGFR(HER1)23 nMW125072WHI-P154≥98%211555-04-310mg,50mgJAK31.8 μMD155111Daphnetin>90.0%(HPLC)486-35-150mg,250mg,1gEGFR7.67 μMPKA9.33 μMPKC25.01 μMP129447PD168393≥98%194423-15-910mg,50mg,250mg EGFR0.70 nMT129439Tyrphostin 9≥98%10537-47-025mg,100mg,500mgEGFR460 μMPDGFR0.5μMT129445Tyrphostin 23≥98%118409-57-710mg,50mg,250mg EGFR35 μMO173511Olmutinib97%1353550-13-6100mgEGFRE107403(-)-表沒食子兒茶素沒食子酸酯分析標準品989-51-520mg,100mg,500mg E107404(-)-表沒食子兒茶素沒食子酸98%989-51-5100mg,500mg,2.5g E126633Erlotinib≥98%183321-74-6100mg,500mg,1g,5g EGFR2 nMN159736Norcantharidin98%29745-04-81g,5g,25gc-MetEGFR B135922Butein≥98.0%(HPLC)487-52-5100mg,1g

*Pim

項目號產品名稱規格CAS包裝細胞靶點IC50
S126376SGI-1776 free base≥98%1025065-69-35mg,10mg,50mg無細胞Pim17 nM
T125988SMI-4a≥98%438190-29-510mg,50mgPim117 nM
A127698AZD1208≥98%1204144-28-45mg,25mg,100mgPim10.4 nM
Pim25 nM
Pim31.9 nM
,

阿拉丁小分子抑制劑、激動劑、拮抗劑--JAK/STAT信號通路

PI3K/AKT/mTOR

JAK/STAT(Janus激酶/信號轉導子和轉錄激活子)信號通路將來自細胞外的化學信號傳遞給細胞核,導致與免疫、增殖、分化、凋亡和腫瘤發生等相關基因的DNA轉錄和表達。此信號通路是眾多細胞因子信號轉導的共同途徑,其活性在炎性疾病和血液惡性腫瘤等疾病治療研究中具有重要意義。JAK-STAT信號級聯由三個主要成分組成:由酪氨酸激酶相關受體、酪氨酸激酶JAK和轉錄因子STAT三個成分組成。

JAK/STAT通路轉導過程

細胞因子,如干擾素、白細胞介素和生長因子等配體,與細胞表面受體結合,引起受體分子二聚化。與受體偶聯的JAK相互接近并通過交互的酪氨酸磷酸化而被激活。活化后的JAK使受體的酪氨酸磷酸化,為具有SH2結構域的STAT創建結合位點。STAT結合至受體后,在JAK作用下,STAT酪氨酸705(Tyr 705)被磷酸化。STAT就會從受體上脫離,形成同/異二聚體。STAT二聚體進入細胞核后,會結合特定的調節序列以激活或抑制靶基因的轉錄。

JAK/STAT信號通路圖

產品列表

按靶點分類:

*JAK

項目號產品名稱規格CAS包裝細胞靶點IC50Ki
R126338Ruxolitinib (INCB018424)≥98%941678-49-55mg,25mg,50mg,100mg無細胞JAK13.3 nM
JAK22.8 nM
E129454Tofacitinib (CP-690550) Citrate≥99%540737-29-910mg,50mg,250mgJAK1112 nM
JAK220 nM
JAK31 nM
A126326AZD1480≥98%935666-88-95mg,25mg,100mg無細胞JAK20.26 nM
T126330Fedratinib (SAR302503, TG101348)≥98%936091-26-85mg,25mg,100mg無細胞JAK23 nM
J126663JANEX-198%202475-60-35mg,10mg,50mg JAK378 μM
W125855WHI-P97≥98%211555-05-410mg,50mgJAK-30.09 μM
C127224CYT387≥98%1056634-68-45mg,10mg,50mg,100mgJAK111 nM
JAK218 nM
T122330Tofacitinib≥98% (HPLC)477600-75-25mg,25mg,100mg,500mg,1g無細胞JAK31 nM
W129459WP1066≥98%857064-38-110mg,50mgHEL細胞JAK22.30 μM
STAT32.43 μM
T127523TG10120998%936091-14-45mg,25mg,100mg無細胞JAK26 nM
Flt325 nM
RET17 nM
L126490LY2784544≥98%1229236-86-55mg,10mg,50mg JAK23 nM
N129609NVP-BSK805 2HCl≥97%1092499-93-85mg,10mg,50mg JAK20.5 nM
B127687Baricitinib≥99%1187594-09-75mg,10mg,50mg無細胞JAK15.9 nM
JAK25.7 nM
A129464AZ 960≥99%905586-69-82mg,5mg,10mg JAK2<3 nM<0.45 nM
C129474CEP-33779≥99%1257704-57-65mg,10mg,50mg JAK21.8 nM
W125072WHI-P154≥98%211555-04-310mg,50mgJAK31.8 μM
X127151XL019≥99%945755-56-6 5mg,25mgJAK22.2 nM
S129613S-Ruxolitinib (INCB018424)≥99%941685-37-65mg,10mg,50mgJAK13.3 nM
JAK22.8 nM
Z129618ZM 39923 HCl≥98%1021868-92-710mg,50mg,250mgJAK14.4
JAK37.1
R171967Ruxolitinib phosphate salt97%1092939-17-7100mgJAK
C114054莪術醇分析標準品,≥98%4871-97-020mg

*STAT

項目號產品名稱規格CAS包裝細胞靶點IC50
S129625S3I-201≥99%501919-59-15mg,10mg,50mg STAT386 μM
F122998氟達拉濱98%21679-14-150mg,250mg,1g,5g STAT1
S129623Stattic≥98%19983-44-925mg,100mg STAT35.1 μM
N130841氯硝柳胺98%50-65-750g,250g無細胞STAT30.7 μM
N114456氯硝柳胺分析標準品50-65-7100mg無細胞STAT30.7 μM
N129550Nifuroxazide≥98%965-52-650mg,100mg STAT1/3/53 μM
A107818青蒿琥酯98%88495-63-05g,25g小細胞肺癌細胞系H69STAT3< 5 μM
C101974隱丹參酮98%35825-57-150mg,250mg無細胞STAT34.6 μM
C101973隱丹參酮分析標準品,≥98%35825-57-120mg無細胞STAT34.6 μM

*EGFR

項目號產品名稱規格CAS包裝細胞靶點IC50Ki
E129310Erlotinib HCl (OSI-744)≥99%183319-69-9100mg,500mg,1g,5g無細胞EGFR2 nM
G125799Gefitinib (ZD1839)≥99%184475-35-250mg,250mg,1g,5g,25g,100gNR6wtEGFR和NR6W細胞Tyr117337 nM
Tyr99237nM
Tyr117326 nM
Tyr99257 nM
L129338二對甲苯磺酸拉帕替尼(GW-572016)≥98%388082-77-725mg,100mg,250mg,500mg,1g無細胞EGFR10.8 nM
ErbB29.2 nM
A129323Afatinib≥99%439081-18-25mg,10mg,50mg無細胞EGFR(wt)0.5 nM
EGFR(L858R)0.4 nM
EGFR(L858R/T790M)10 nM
ErbB2(HER2)14 nM
ErbB4(HER4)1 nM
N126132Neratinib (HKI-272)≥99%698387-09-65mg,25mg,100mg無細胞HER259 nM
EGFR92 nM
P125741PD153035≥98%153436-54-510mg,50mg,250mg EGFR5.2 pM
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