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首页 >  新闻动态 >  阿拉丁小分子抑制剂、激动剂、拮抗剂--JAK/STAT信号通路

阿拉丁小分子抑制剂、激动剂、拮抗剂--JAK/STAT信号通路

发布时间:2019-12-09

阿拉丁小分子抑制剂、激动剂、拮抗剂--JAK/STAT信号通路

PI3K/AKT/mTOR

JAK/STAT(Janus激酶/信号转导子和转录激活子)信号通路将来自细胞外的化学信号传递给细胞核,导致与免疫、增殖、分化、凋亡和肿瘤发生等相关基因的DNA转录和表达。此信号通路是众多细胞因子信号转导的共同途径,其活性在炎性疾病和血液恶性肿瘤等疾病治疗研究中具有重要意义。JAK-STAT信号级联由三个主要成分组成:由酪氨酸激酶相关受体、酪氨酸激酶JAK和转录因子STAT三个成分组成。

JAK/STAT通路转导过程

细胞因子,如干扰素、白细胞介素和生长因子等配体,与细胞表面受体结合,引起受体分子二聚化。与受体偶联的JAK相互接近并通过交互的酪氨酸磷酸化而被激活。活化后的JAK使受体的酪氨酸磷酸化,为具有SH2结构域的STAT创建结合位点。STAT结合至受体后,在JAK作用下,STAT酪氨酸705(Tyr 705)被磷酸化。STAT就会从受体上脱离,形成同/异二聚体。STAT二聚体进入细胞核后,会结合特定的调节序列以激活或抑制靶基因的转录。

JAK/STAT信号通路图

产品列表

按靶点分类:     

*JAK

项目号产品名称规格CAS包装细胞靶点IC50Ki
R126338Ruxolitinib (INCB018424)≥98%941678-49-55mg,25mg,50mg,100mg无细胞JAK13.3 nM
JAK22.8 nM
E129454Tofacitinib (CP-690550) Citrate≥99%540737-29-910mg,50mg,250mg
JAK1112 nM
JAK220 nM
JAK31 nM
A126326AZD1480≥98%935666-88-95mg,25mg,100mg无细胞JAK20.26 nM
T126330Fedratinib (SAR302503, TG101348)≥98%936091-26-85mg,25mg,100mg无细胞JAK23 nM
J126663JANEX-198%202475-60-35mg,10mg,50mg
JAK378 μM
W125855WHI-P97≥98%211555-05-410mg,50mg
JAK-3
0.09 μM
C127224CYT387≥98%1056634-68-45mg,10mg,50mg,100mg
JAK111 nM
JAK218 nM
T122330Tofacitinib≥98% (HPLC)477600-75-25mg,25mg,100mg,500mg,1g无细胞JAK31 nM
W129459WP1066≥98%857064-38-110mg,50mgHEL细胞JAK22.30 μM
STAT32.43 μM
T127523TG10120998%936091-14-45mg,25mg,100mg无细胞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无细胞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,50mg
JAK31.8 μM
X127151XL019≥99%945755-56-6 5mg,25mg
JAK22.2 nM
S129613S-Ruxolitinib (INCB018424)≥99%941685-37-65mg,10mg,50mg
JAK13.3 nM
JAK22.8 nM
Z129618ZM 39923 HCl≥98%1021868-92-710mg,50mg,250mg
JAK14.4
JAK37.1
R171967Ruxolitinib phosphate salt97%1092939-17-7100mg
JAK

C114054莪术醇分析标准品,≥98%4871-97-020mg



 

*STAT

项目号产品名称规格CAS包装细胞靶点IC50
S129625S3I-201≥99%501919-59-15mg,10mg,50mg
STAT386 μM
F122998氟达拉滨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无细胞STAT30.7 μM
N114456氯硝柳胺分析标准品50-65-7100mg无细胞STAT30.7 μM
N129550Nifuroxazide≥98%965-52-650mg,100mg
STAT1/3/53 μM
A107818青蒿琥酯98%88495-63-05g,25g小细胞肺癌细胞系H69STAT3< 5 μM
C101974隐丹参酮98%35825-57-150mg,250mg无细胞STAT34.6 μM
C101973隐丹参酮分析标准品,≥98%35825-57-120mg无细胞STAT34.6 μM

 

*EGFR

项目号产品名称规格CAS包装细胞靶点IC50Ki
E129310Erlotinib HCl (OSI-744)≥99%183319-69-9100mg,500mg,1g,5g无细胞EGFR2 nM
G125799Gefitinib (ZD1839)≥99%184475-35-250mg,250mg,1g,5g,25g,100gNR6wtEGFR和NR6W细胞Tyr117337 nM
Tyr99237nM
Tyr117326 nM
Tyr99257 nM
L129338二对甲苯磺酸拉帕替尼(GW-572016)≥98%388082-77-725mg,100mg,250mg,500mg,1g无细胞EGFR10.8 nM
ErbB29.2 nM
A129323Afatinib≥99%439081-18-25mg,10mg,50mg无细胞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无细胞HER259 nM
EGFR92 nM
P125741PD153035≥98%153436-54-510mg,50mg,250mg
EGFR
5.2 pM
T162509酪氨酸激酶抑制剂 AG 494>98.0%(HPLC)(N)133550-35-320mg,100mg
EGFR1.2 μM
EGF6 μM
C125447Canertinib (CI-1033)≥98%267243-28-710mg,50mg,250mg
EGFR1.5 nM
ErbB29.0 nM
L126696Lapatinib≥99%231277-92-225mg,100mg,250mg,500mg,1g,5g无细胞EGFR10.2 nM
ErbB29.8 nM
A126525AG-490 (Tyrphostin B42)≥98%133550-30-820mg,50mg,250mg,1g无细胞EGFR0.1 μM
C129397CP-724714≥99%537705-08-15mg,10mg,25mg,50mg
HER2/ErbB210 nM
D129347Dacomitinib (PF299804, PF299)≥99%1110813-31-45mg,10mg,50mg,250mg无细胞EGFR6 nM
W127713WZ4002≥98%1213269-23-810mg,50mg,100mgBaF3细胞系EGFR(L858R)2 nM
EGFR(T790M)8 nM
A129380AZD8931 (Sapitinib)≥98%848942-61-05mg,10mg,50mg
EGFR4 nM
ErbB23 nM
ErbB34 nM
C127191CUDC-101≥98%1012054-59-910mg,25mg,50mg,100mg,250mg
HDAC4.4 nM
EGFR2.4 nM
HER215.7 nM
A126582AG-1478 (Tyrphostin AG-1478)≥98%153436-53-45mg,10mg,25mg,50mg无细胞EGFR3 nM
P129384PD153035 HCl≥98%(HPLC)183322-45-410mg,50mg,250mg
EGFR29 pM5.2 pM
P125444Pelitinib≥98%257933-82-75mg,25mg,100mg
EGFR38.5 nM
B126145AC480 (BMS-599626)≥98%714971-09-25mg,25mg,100mg
HER120 nM
HER230 nM
A126830AEE788 (NVP-AEE788)≥97%497839-62-05mg,25mg,100mg
EGFR2 nM
HER2/ErbB26 nM
A127691AP26113≥98%1197958-12-55mg,10mg,25mg,50mg,100mg
ALK


EGFR

O125033OSI-420≥99%183320-51-65mg,10mg,50mg
EGFR2 nM
W127717WZ3146≥98%1214265-56-15mg,25mg,100mg
EGFR(L858R)2 nM
EGFR(E746_A750)2 nM
A126334ARRY-380≥98%937265-83-35mg,10mg,50mg
HER28 nM
W126471WZ8040≥98%1214265-57-25mg,25mg,50mg
EGFRT790M
A129426AST-1306 TsOH≥98%1050500-29-25mg,10mg,50mg
EGFR0.5 nM
ErbB23 nM
C124905CO-1686 (AVL-301)≥99%1374640-70-65mg,10mg,50mg,100mg无细胞EGFRL858R/T790M21.5 nM
EGFRWT
303.3 nM
G106672金雀异黄酮分析标准品,≥98%446-72-020mg,1g,5gNIH-3T3细胞EGF12μM
胰岛素19 μM
G106673金雀异黄酮97%446-72-0100mg,500mg,1g,5g,25gNIH-3T3细胞EGF12μM
胰岛素19 μM
V129433Varlitinib≥96%845272-21-15mg,10mg,50mg
ErbB1(EGFR)7 nM
ErbB2(HER2)2 nM
I129405Icotinib≥99%610798-31-75mg,10mg,50mg
EGFR5 nM
T126234TAK-285≥98%871026-44-75mg,10mg,50mg
HER2和EGFR(HER1)17 nM
HER2和EGFR(HER1)23 nM
W125072WHI-P154≥98%211555-04-310mg,50mg
JAK31.8 μM
D155111Daphnetin>90.0%(HPLC)486-35-150mg,250mg,1g
EGFR7.67 μM
PKA9.33 μM
PKC25.01 μM
P129447PD168393≥98%194423-15-910mg,50mg,250mg
EGFR0.70 nM
T129439Tyrphostin 9≥98%10537-47-025mg,100mg,500mg
EGFR460 μM
PDGFR0.5μM
T129445Tyrphostin 23≥98%118409-57-710mg,50mg,250mg
EGFR35 μM
O173511Olmutinib97%1353550-13-6100mg
EGFR

E107403(-)-表没食子儿茶素没食子酸酯分析标准品989-51-520mg,100mg,500mg



E107404(-)-表没食子儿茶素没食子酸98%989-51-5100mg,500mg,2.5g



E126633Erlotinib≥98%183321-74-6100mg,500mg,1g,5g
EGFR2 nM
N159736Norcantharidin98%29745-04-81g,5g,25g
c-Met


EGFR 

B135922Butein≥98.0%(HPLC)487-52-5100mg,1g



 

*Pim

项目号产品名称规格CAS包装细胞靶点IC50
S126376SGI-1776 free base≥98%1025065-69-35mg,10mg,50mg无细胞Pim17 nM
T125988SMI-4a≥98%438190-29-510mg,50mg
Pim117 nM
A127698AZD1208≥98%1204144-28-45mg,25mg,100mg
Pim10.4 nM
Pim25 nM
Pim31.9 nM


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