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阿拉丁小分子抑制剂、激动剂、拮抗剂--JAK/STAT信号通路

2019-12-09

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	IC50	Ki
R126338	Ruxolitinib (INCB018424)	≥98%	941678-49-5	5mg,25mg,50mg,100mg	无细胞	JAK1	3.3 nM
R126338	Ruxolitinib (INCB018424)	≥98%	941678-49-5	5mg,25mg,50mg,100mg	无细胞	JAK2	2.8 nM
E129454	Tofacitinib (CP-690550) Citrate	≥99%	540737-29-9	10mg,50mg,250mg		JAK1	112 nM
						JAK2	20 nM
						JAK3	1 nM
A126326	AZD1480	≥98%	935666-88-9	5mg,25mg,100mg	无细胞	JAK2	0.26 nM
T126330	Fedratinib (SAR302503, TG101348)	≥98%	936091-26-8	5mg,25mg,100mg	无细胞	JAK2	3 nM
J126663	JANEX-1	98%	202475-60-3	5mg,10mg,50mg		JAK3	78 μM
W125855	WHI-P97	≥98%	211555-05-4	10mg,50mg		JAK-3		0.09 μM
C127224	CYT387	≥98%	1056634-68-4	5mg,10mg,50mg,100mg		JAK1	11 nM
C127224	CYT387	≥98%	1056634-68-4	5mg,10mg,50mg,100mg		JAK2	18 nM
T122330	Tofacitinib	≥98% (HPLC)	477600-75-2	5mg,25mg,100mg,500mg,1g	无细胞	JAK3	1 nM
W129459	WP1066	≥98%	857064-38-1	10mg,50mg	HEL细胞	JAK2	2.30 μM
W129459	WP1066	≥98%	857064-38-1	10mg,50mg	HEL细胞	STAT3	2.43 μM
T127523	TG101209	98%	936091-14-4	5mg,25mg,100mg	无细胞	JAK2	6 nM
						Flt3	25 nM
						RET	17 nM
L126490	LY2784544	≥98%	1229236-86-5	5mg,10mg,50mg		JAK2	3 nM
N129609	NVP-BSK805 2HCl	≥97%	1092499-93-8	5mg,10mg,50mg		JAK2	0.5 nM
B127687	Baricitinib	≥99%	1187594-09-7	5mg,10mg,50mg	无细胞	JAK1	5.9 nM
B127687	Baricitinib	≥99%	1187594-09-7	5mg,10mg,50mg	无细胞	JAK2	5.7 nM
A129464	AZ 960	≥99%	905586-69-8	2mg,5mg,10mg		JAK2	＜3 nM	＜0.45 nM
C129474	CEP-33779	≥99%	1257704-57-6	5mg,10mg,50mg		JAK2	1.8 nM
W125072	WHI-P154	≥98%	211555-04-3	10mg,50mg		JAK3	1.8 μM
X127151	XL019	≥99%	945755-56-6	5mg,25mg		JAK2	2.2 nM
S129613	S-Ruxolitinib (INCB018424)	≥99%	941685-37-6	5mg,10mg,50mg		JAK1	3.3 nM
S129613	S-Ruxolitinib (INCB018424)	≥99%	941685-37-6	5mg,10mg,50mg		JAK2	2.8 nM
Z129618	ZM 39923 HCl	≥98%	1021868-92-7	10mg,50mg,250mg		JAK1	4.4
Z129618	ZM 39923 HCl	≥98%	1021868-92-7	10mg,50mg,250mg		JAK3	7.1
R171967	Ruxolitinib phosphate salt	97%	1092939-17-7	100mg		JAK
C114054	莪术醇	分析标准品,≥98%	4871-97-0	20mg

*STAT

项目号	产品名称	规格	CAS	包装	细胞	靶点	IC50
S129625	S3I-201	≥99%	501919-59-1	5mg,10mg,50mg		STAT3	86 μM
F122998	氟达拉滨	98%	21679-14-1	50mg,250mg,1g,5g		STAT1
S129623	Stattic	≥98%	19983-44-9	25mg,100mg		STAT3	5.1 μM
N130841	氯硝柳胺	98%	50-65-7	50g,250g	无细胞	STAT3	0.7 μM
N114456	氯硝柳胺	分析标准品	50-65-7	100mg	无细胞	STAT3	0.7 μM
N129550	Nifuroxazide	≥98%	965-52-6	50mg,100mg		STAT1/3/5	3 μM
A107818	青蒿琥酯	98%	88495-63-0	5g,25g	小细胞肺癌细胞系H69	STAT3	< 5 μM
C101974	隐丹参酮	98%	35825-57-1	50mg,250mg	无细胞	STAT3	4.6 μM
C101973	隐丹参酮	分析标准品,≥98%	35825-57-1	20mg	无细胞	STAT3	4.6 μM

*EGFR

项目号	产品名称	规格	CAS	包装	细胞	靶点	IC50	Ki
E129310	Erlotinib HCl (OSI-744)	≥99%	183319-69-9	100mg,500mg,1g,5g	无细胞	EGFR	2 nM
G125799	Gefitinib (ZD1839)	≥99%	184475-35-2	50mg,250mg,1g,5g,25g,100g	NR6wtEGFR和NR6W细胞	Tyr1173	37 nM
						Tyr992	37nM
						Tyr1173	26 nM
						Tyr992	57 nM
L129338	二对甲苯磺酸拉帕替尼(GW-572016)	≥98%	388082-77-7	25mg,100mg,250mg,500mg,1g	无细胞	EGFR	10.8 nM
L129338	二对甲苯磺酸拉帕替尼(GW-572016)	≥98%	388082-77-7	25mg,100mg,250mg,500mg,1g	无细胞	ErbB2	9.2 nM
A129323	Afatinib	≥99%	439081-18-2	5mg,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
N126132	Neratinib (HKI-272)	≥99%	698387-09-6	5mg,25mg,100mg	无细胞	HER2	59 nM
N126132	Neratinib (HKI-272)	≥99%	698387-09-6	5mg,25mg,100mg	无细胞	EGFR	92 nM
P125741	PD153035	≥98%	153436-54-5	10mg,50mg,250mg		EGFR		5.2 pM
T162509	酪氨酸激酶抑制剂 AG 494	>98.0%(HPLC)(N)	133550-35-3	20mg,100mg		EGFR	1.2 μM
T162509	酪氨酸激酶抑制剂 AG 494	>98.0%(HPLC)(N)	133550-35-3	20mg,100mg		EGF	6 μM
C125447	Canertinib (CI-1033)	≥98%	267243-28-7	10mg,50mg,250mg		EGFR	1.5 nM
C125447	Canertinib (CI-1033)	≥98%	267243-28-7	10mg,50mg,250mg		ErbB2	9.0 nM
L126696	Lapatinib	≥99%	231277-92-2	25mg,100mg,250mg,500mg,1g,5g	无细胞	EGFR	10.2 nM
L126696	Lapatinib	≥99%	231277-92-2	25mg,100mg,250mg,500mg,1g,5g	无细胞	ErbB2	9.8 nM
A126525	AG-490 (Tyrphostin B42)	≥98%	133550-30-8	20mg,50mg,250mg,1g	无细胞	EGFR	0.1 μM
C129397	CP-724714	≥99%	537705-08-1	5mg,10mg,25mg,50mg		HER2/ErbB2	10 nM
D129347	Dacomitinib (PF299804, PF299)	≥99%	1110813-31-4	5mg,10mg,50mg,250mg	无细胞	EGFR	6 nM
W127713	WZ4002	≥98%	1213269-23-8	10mg,50mg,100mg	BaF3细胞系	EGFR(L858R)	2 nM
W127713	WZ4002	≥98%	1213269-23-8	10mg,50mg,100mg	BaF3细胞系	EGFR(T790M)	8 nM
A129380	AZD8931 (Sapitinib)	≥98%	848942-61-0	5mg,10mg,50mg		EGFR	4 nM
						ErbB2	3 nM
						ErbB3	4 nM
C127191	CUDC-101	≥98%	1012054-59-9	10mg,25mg,50mg,100mg,250mg		HDAC	4.4 nM
						EGFR	2.4 nM
						HER2	15.7 nM
A126582	AG-1478 (Tyrphostin AG-1478)	≥98%	153436-53-4	5mg,10mg,25mg,50mg	无细胞	EGFR	3 nM
P129384	PD153035 HCl	≥98%(HPLC)	183322-45-4	10mg,50mg,250mg		EGFR	29 pM	5.2 pM
P125444	Pelitinib	≥98%	257933-82-7	5mg,25mg,100mg		EGFR	38.5 nM
B126145	AC480 (BMS-599626)	≥98%	714971-09-2	5mg,25mg,100mg		HER1	20 nM
B126145	AC480 (BMS-599626)	≥98%	714971-09-2	5mg,25mg,100mg		HER2	30 nM
A126830	AEE788 (NVP-AEE788)	≥97%	497839-62-0	5mg,25mg,100mg		EGFR	2 nM
A126830	AEE788 (NVP-AEE788)	≥97%	497839-62-0	5mg,25mg,100mg		HER2/ErbB2	6 nM
A127691	AP26113	≥98%	1197958-12-5	5mg,10mg,25mg,50mg,100mg		ALK
A127691	AP26113	≥98%	1197958-12-5	5mg,10mg,25mg,50mg,100mg		EGFR
O125033	OSI-420	≥99%	183320-51-6	5mg,10mg,50mg		EGFR	2 nM
W127717	WZ3146	≥98%	1214265-56-1	5mg,25mg,100mg		EGFR(L858R)	2 nM
W127717	WZ3146	≥98%	1214265-56-1	5mg,25mg,100mg		EGFR(E746_A750)	2 nM
A126334	ARRY-380	≥98%	937265-83-3	5mg,10mg,50mg		HER2	8 nM
W126471	WZ8040	≥98%	1214265-57-2	5mg,25mg,50mg		EGFRT790M
A129426	AST-1306 TsOH	≥98%	1050500-29-2	5mg,10mg,50mg		EGFR	0.5 nM
A129426	AST-1306 TsOH	≥98%	1050500-29-2	5mg,10mg,50mg		ErbB2	3 nM
C124905	CO-1686 (AVL-301)	≥99%	1374640-70-6	5mg,10mg,50mg,100mg	无细胞	EGFRL858R/T790M		21.5 nM
C124905	CO-1686 (AVL-301)	≥99%	1374640-70-6	5mg,10mg,50mg,100mg	无细胞	EGFRWT		303.3 nM
G106672	金雀异黄酮	分析标准品,≥98%	446-72-0	20mg,1g,5g	NIH-3T3细胞	EGF	12μM
G106672	金雀异黄酮	分析标准品,≥98%	446-72-0	20mg,1g,5g	NIH-3T3细胞	胰岛素	19 μM
G106673	金雀异黄酮	97%	446-72-0	100mg,500mg,1g,5g,25g	NIH-3T3细胞	EGF	12μM
G106673	金雀异黄酮	97%	446-72-0	100mg,500mg,1g,5g,25g	NIH-3T3细胞	胰岛素	19 μM
V129433	Varlitinib	≥96%	845272-21-1	5mg,10mg,50mg		ErbB1(EGFR)	7 nM
V129433	Varlitinib	≥96%	845272-21-1	5mg,10mg,50mg		ErbB2(HER2)	2 nM
I129405	Icotinib	≥99%	610798-31-7	5mg,10mg,50mg		EGFR	5 nM
T126234	TAK-285	≥98%	871026-44-7	5mg,10mg,50mg		HER2和EGFR(HER1)	17 nM
T126234	TAK-285	≥98%	871026-44-7	5mg,10mg,50mg		HER2和EGFR(HER1)	23 nM
W125072	WHI-P154	≥98%	211555-04-3	10mg,50mg		JAK3	1.8 μM
D155111	Daphnetin	>90.0%(HPLC)	486-35-1	50mg,250mg,1g		EGFR	7.67 μM
						PKA	9.33 μM
						PKC	25.01 μM
P129447	PD168393	≥98%	194423-15-9	10mg,50mg,250mg		EGFR	0.70 nM
T129439	Tyrphostin 9	≥98%	10537-47-0	25mg,100mg,500mg		EGFR	460 μM
T129439	Tyrphostin 9	≥98%	10537-47-0	25mg,100mg,500mg		PDGFR	0.5μM
T129445	Tyrphostin 23	≥98%	118409-57-7	10mg,50mg,250mg		EGFR	35 μM
O173511	Olmutinib	97%	1353550-13-6	100mg		EGFR
E107403	(-)-表没食子儿茶素没食子酸酯	分析标准品	989-51-5	20mg,100mg,500mg
E107404	(-)-表没食子儿茶素没食子酸	98%	989-51-5	100mg,500mg,2.5g
E126633	Erlotinib	≥98%	183321-74-6	100mg,500mg,1g,5g		EGFR	2 nM
N159736	Norcantharidin	98%	29745-04-8	1g,5g,25g		c-Met
N159736	Norcantharidin	98%	29745-04-8	1g,5g,25g		EGFR
B135922	Butein	≥98.0%(HPLC)	487-52-5	100mg,1g

*Pim

项目号	产品名称	规格	CAS	包装	细胞	靶点	IC50
S126376	SGI-1776 free base	≥98%	1025065-69-3	5mg,10mg,50mg	无细胞	Pim1	7 nM
T125988	SMI-4a	≥98%	438190-29-5	10mg,50mg		Pim1	17 nM
A127698	AZD1208	≥98%	1204144-28-4	5mg,25mg,100mg		Pim1	0.4 nM
						Pim2	5 nM
						Pim3	1.9 nM