TG101209 | JAK2 Inhibitor | AmBeed-信号通路专用抑制剂

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TG101209 99%+

货号：A469558

TG 101209 is a potent and selective JAK2 inhibitor with IC50 of 6 nM, also inhibits Flt3 and RET with IC50 values of 25 nM and 17 nM, respectively.

TG101209 化学结构
CAS号：936091-14-4

TG101209 3D分子结构
CAS号：936091-14-4

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TG101209 纯度/质量文件产品仅供科研

货号：A469558 标准纯度： 99%+ 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Cell,2024. Ambeed. [ A125712 ]; • Cancer Discov., 2024. Ambeed. [ A285925 ]; • JMC, 2024. Ambeed. [ A288696 ]; • JMC, 2024. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]; • EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]; 更多 >

表观遗传阅读框亚型比较
c-RET 亚型比较
JAK 亚型比较
FLT3 亚型比较

产品名称	BET ↓ ↑	bromodomain ↓ ↑	BRPF ↓ ↑	CBP/beta-catenin ↓ ↑	p300/CBP ↓ ↑	其他靶点	纯度
MS436	++ BRD4 (1), Ki: <0.085 μM BRD4 (2), Ki: 0.34 μM						99%+
CPI-203	+++ BRD4, IC50: 37 nM						99+%
GSK1324726A	+++ BRD4, IC50: 22 nM BRD2, IC50: 31 nM						99%+
PFI-1	++ BRD4, IC50: 0.22 μM BRD2, IC50: 98 nM						99%+
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (1), IC50: 77 nM BRD4 (2), IC50: 33 nM						99%+
I-BET151	+ BRD4, IC50: 0.5 μM BRD3, IC50: 0.25 μM						99%+
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD4, pIC50: 5.3 BRD9, pIC50: 7.3						99%+
BI-7273	++++ BRD7, IC50: 117 nM BRD9, IC50: 19 nM						99+%
Pelabresib	+++ BRD4-BD1, IC50: 39 nM						98%
ARV-825	+++ BRD4 BD2, Kd: 28 nM BRD4 BD1, Kd: 90 nM						99%+
Birabresib							99%+
BI 2536	+++ BRD4, Kd: 37 nM					c-Myc	99%+
Bromosporine	++ BRD9, IC50: 0.122 μM BRD2, IC50: 0.29 μM	++++ CECR2, IC50: 17 nM					99%+
XMD8-92	++ BRD4 (1), Kd: 170 nM						99%+
Mivebresib	✔						99%+
BI-9564	++++ BRD7, Kd: 73 nM BRD9, Kd: 5.9 nM	++ CECR2, Kd: 77 nM					99%+
AZD5153 6-Hydroxy-2-naphthoic acid	++++ FL-BRD4, IC50: 5 nM						99%+
PLX51107	++++ BRD3 BD1, Kd: 2.1 nM BRD4 BD2, Kd: 1.7 nM						99%+
FL-411	+ BRD4(1), IC50: 0.43 μM						99%+
ABBV-744	✔						99%+
dBET6	++++ BRD4, IC50: 14 nM						99%+
dBET1	++++ BRD4, IC50: 20 nM						99%+
MZ1	++++ Brd2(BD2), Kd: 62 nM Brd3(BD2), Kd: 13 nM						99%+
dBET57	+ BRD4_BD1, DC50: 500 nM						99%+
SF2523	+ BRD4, IC50: 241 nM					DNA-PK	99%+
INCB054329	++++ BRD4-BD1, IC50: 119 nM BRD3-BD1, IC50: 9 nM						99%
INCB-057643	✔						99%+
(E/Z)-ZL0420	+++ BRD4 BD1, IC50: 27 nM BRD4 BD2, IC50: 32 nM						99%+
BMS-986158	✔						99%+
BRD4 Inhibitor-10	++++ BRD4-BD2, IC50: 41 nM BRD4-BD1, IC50: 5 nM						97%
A1874	✔						99%+
Y06036	++ BRD4 (1), Kd: 82 nM						99%+
Alobresib	✔					NF-κB	98%
ODM-207	✔						99%
GSK778	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						97%
SRX3207	+ BRD41, IC50: 3070 nM BRD42, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD3_BD2, IC50: 98 nM BRD4_BD2, IC50: 214 nM						98%
GSK620	✔						97%
Thalidomide-NH-C4-NH-Boc	✔						98%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						99%+
GSK2801		++ BAZ2B, Kd: 136 nM BAZ2A, Kd: 257 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL3, IC50: 35 μM L3MBTL4, IC50: 6 μM					99%+
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 nM					99%+
UNC1215		+++ L3MBTL3- D274A, IC50: 3.5 μM L3MBTL3, IC50: 120 nM					99%+
EED226		++ EED, Kd: 82 nM PRC2, Kd: 114 nM					99%+
BRD9539		✔					99%+
UNC926		+ L3MBTL1, Kd: 3.9 μM					99%
666-15		++ CREB, IC50: 81 nM					99%+
UNC6852		+ EED, IC50: 247 nM					99%+
BAZ1A-IN-1		+ BAZ1A, Kd: 0.52 μM					99%+
PFI-4			++ BRPF2, IC50: 7.9 μM BRPF1, IC50: 80 nM				99%+
OF-1			++ BRPF2, Kd: 500 nM BRPF1B, Kd: 100 nM				99%+
GSK-5959			++ BRPF2, pIC50: 5.2 BRPF3, pIC50: 7.1				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF3, IC50: 260 nM BRPF1, IC50: 48 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			99%+
I-CBP112					++ p300, Kd: 167 nM CBP, Kd: 151 nM		98+%
Histone Acetyltransferase Inhibitor II					+ p300, IC50: 5 μM		99%+
C646					+ p300/CBP, Ki: 400 nM		99%+
Anacardic Acid					+ PCAF, IC50: 5 μM p300/CBP, IC50: 8.5 μM		99%+
SGC-CBP30					++++ CREBBP, IC50: 21 nM EP300, IC50: 38 nM		99%+
Nordihydroguaiaretic acid					✔	IGF-1R,HER2	99%+
Curcumin					+ p300, IC50: ~25 μM	Ferroptosis,Nrf2,NF-κB	98%
PF-CBP1 HCl					++ p300/CBP, IC50: 363nM CREBBP, IC50: 125nM		97%
CPI-637					+++ EP300, IC50: 0.051 μM CBP, IC50: 0.03 μM		99%+
Foscenvivint					✔	β-catenin	99%+
A-485					++ p300 HAT, IC50: 0.06 μM		99%+
GNE-781	+ BRD4(1), IC50: 5100 nM				++++ CBP, IC50: 0.94 nM		99%+
NEO2734	+++ BET, IC50: <30 nM				+++ p300/CBP, IC50: <30 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	c-RET ↓ ↑	其他靶点	纯度
Regorafenib	+++ RET, IC50: 1.5 nM		98%
TG101209	++ RET, IC50: 17 nM	FLT3	99%+
Danusertib	+ RET, IC50: 31 nM		99%+
AD80	++++ RET V804M, IC50: 0.6 nM RET wt, IC50: 1.3 nM	Raf,Src	99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	JAK1 ↓ ↑	JAK2 ↓ ↑	JAK3 ↓ ↑	Tyk2 ↓ ↑	其他靶点	纯度
Decernotinib	+++ JAK1, IC50: 11 nM JAK1, Ki: 11 nM	+++ JAK2, Ki: 13 nM	++++ JAK3, Ki: 2.5 nM	+++ TYK2, Ki: 13 nM		99%+
ZM39923 HCl	+ JAK1, pIC50: 4.4		+ JAK3, pIC50: 7.1		EGFR	97%
Cerdulatinib	+++ JAK1, IC50: 12 nM	+++ JAK2, IC50: 6 nM	+++ JAK3, IC50: 8 nM	++++ TYK2, IC50: 0.5 nM		99%+
Momelotinib	+++ JAK1, IC50: 11 nM	++ JAK2, IC50: 18 nM	+ JAK3, IC50: 155 nM			99%+
XL019	+ JAK1, IC50: 134.3 nM	++++ JAK2, IC50: 2.2 nM	+ JAK3, IC50: 214.2 nM		FLT3	99%+
Ruxolitinib	+++ JAK1, IC50: 3.3 nM	++++ JAK2, IC50: 2.8 nM				99%+
Tofacitinib	+ JAK1, IC50: 112 nM	++ JAK2, IC50: 20 nM	++++ JAK3, IC50: 1 nM			98%
Ruxolitinib (S enantiomer)	+++ JAK1, IC50: 3.3 nM	++++ JAK2, IC50: 2.8 nM		++ TYK2, IC50: 19 nM		98%
Filgotinib	+++ JAK1, IC50: 10 nM	++ JAK2, IC50: 28 nM	+ JAK3, IC50: 810 nM	+ TYK2, IC50: 116 nM		99%
Baricitinib	+++ JAK1, IC50: 5.9 nM	+++ JAK2, IC50: 5.7 nM		++ TYK2, IC50: 53 nM		99%
Gandotinib	++ JAK1, IC50: 19.8 nM	++++ JAK2 (V617F), Ki: 0.245 nM JAK2, IC50: 0.288 nM	++ JAK3, IC50: 48.0 nM	++ TYK2, IC50: 44 nM	FLT3	99%+
Oclacitinib maleate	+++ JAK1, IC50: 10nM	++ JAK2, IC50: 18nM	+ JAK3, IC50: 99nM	+ TYK2, IC50: 84nM		98+%
NVP-BSK805 2HCl	++ JAK1, IC50: 31.63 nM	++++ JAK2, IC50: ~0.5 nM	++ JAK3, IC50: 18.68 nM	+++ TYK2, IC50: 10.76 nM		99+%
Peficitinib		✔				98%
Go6976		✔			FLT3	99%+
AZD-1480		++++ JAK2, IC50: 0.26 nM				99%+
Fedratinib		+++ JAK2 (V617F), IC50: 3 nM JAK2, IC50: 3 nM			RET,FLT3	99%+
WP1066		+ JAK2, IC50: 2.3 μM				99%+
Curcumol		✔				98%
AZ960		++++ JAK2, IC50: <3 nM JAK2, Ki: 0.45 nM				98%+
GLPG0634 analog		✔				99%+
CEP-33779		++++ JAK2, IC50: 1.8 nM				99%+
FLLL32		+ JAK2, IC50: <5 μM				99%+
WHI-P154			+ JAK3, IC50: 1.8 μM		VEGFR,Src,EGFR	99%+
BMS-911543		++++ JAK2, IC50: 1.1 nM	+ JAK3, IC50: 75 nM	++ TYK2, IC50: 66 nM		98%
TG101209		+++ JAK2, IC50: 6 nM	+ JAK3, IC50: 169 nM		RET,FLT3	99%+
AT9283		++++ JAK2, IC50: 1.2 nM	++++ JAK3, IC50: 1.1 nM			99%+
Pacritinib		++ JAK2 (V617F), IC50: 19 nM JAK2, IC50: 23 nM	+ JAK3, IC50: 520 nM	++ TYK2, IC50: 50 nM	FLT3	97%
Tofacitinib citrate		++ JAK2, IC50: 20 nM	++++ JAK3, IC50: 1 nM			99%
FM-381			++++ JAK3, IC50: 127 pM			99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	FLT3 ↓ ↑	其他靶点	纯度
R406	✔	Syk	99%+
Go6976	✔		99%+
Quizartinib	+++ FLT3 (ITD), IC50: 1.1 nM FLT3 (WT), IC50: 4.2 nM		99%+
Gilteritinib	++++ FLT3, IC50: 0.29 nM		99%+
Amuvatinib	+ FLT3 (D835Y), IC50: 81 nM		99%+
Pacritinib	++ FLT3 (D835Y), IC50: 6 nM FLT3, IC50: 22 nM		97%
Dovitinib	++++ FLT3, IC50: 1 nM	c-Kit	99%+
Denfivontinib	++++ FLT3 (D835Y), IC50: 0.4 nM FLT3, IC50: 0.4 nM	RET	99%+
TAK-659 HCl	++ FLT3, IC50: 4.6 nM	Syk	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

TG101209 生物活性

靶点	JAK3 JAK3, IC50:169 nM JAK2 JAK2, IC50:6 nM c-RET RET, IC50:17 nM
描述	Janus kinase 2 (JAK2) is a tyrosine kinase associated with the pathogenesis of myeloproliferative disorders. TG 101209 is a potent, orally bioavailable, small-molecule JAK2 inhibitor with an IC50 value of 6nM. It exhibits 28-fold potency for JAK2 relative to JAK3 in vitro. TG 101209 also shows inhibitory activities against FLT3 and RET with IC50 values of 25 and 17nM, respectively. TG 101209 inhibited the growth of Ba/F3-V617F and Ba/F3-W515L cells with IC50 values of 170 and 220 nM, respectively, but only had minimal effect on CTLL-2 cell growth with an IC50 value of 3400nM. In HEL cells homozygous for the JAK2V617F allele, treatment with TG 101209 at 4.6-38400nM resulted in a concentration-dependent inhibition of cell growth with an IC50 value of 152nM. TG 101209 also potently inhibited the proliferation of CHRF-288-11 cells with an IC50 value of 16nM. HEL cells treated with 600nM TG 101209 showed an increased percentage of Annexin V-positive cells compared to the background level at 24, 48, and 72h. Treatment of HEL cells with 1200nM TG 101209 for 24h increased the percentage of G0/G1 fraction cells compared with the background level. TG 101209 inhibited STAT5 phosphorylation in Ba/F3-V617F cells with an IC50 value of ~300nM. In a mouse model of JAK2V617F-induced hematopoietic disease, oral administration of TG 101209 (100mg/kg, b.i.d) for 10 days significantly prolonged the survival of animals compared with the vehicle-treated group^[3].
作用机制	TG 101209 is a potent, selective JAK2 inhibitor. It docked and minimized in the ATP pocket of JAK2. TG 101209 effectively inhibited JAK2V617F and MPLW515L/K tyrosine kinases both in vitro and in vivo^[3].

TG101209 参考文献

[1]Ma AC, Fan A, et al. A novel zebrafish jak2a(V581F) model shared features of human JAK2(V617F) polycythemia vera. Exp Hematol. 2009 Dec;37(12):1379-1386.e4.

[2]Pardanani A, Hood J, et al. TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia. 2007 Aug;21(8):1658-68.

[3]Pardanani A, Hood J, Lasho T, et al. TG101209, a small molecule JAK2-selective kinase inhibitor potently inhibits myeloproliferative disorder-associated JAK2V617F and MPLW515L/K mutations. Leukemia. 2007;21(8):1658-1668. doi:10.1038/sj.leu.2404750

TG101209 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.96mL

0.39mL

0.20mL

9.81mL

1.96mL

0.98mL

19.62mL

3.92mL

1.96mL

TG101209 技术信息

CAS号	936091-14-4
分子式	C₂₆H₃₅N₇O₂S
分子量	509.667

别名
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(98.1 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+30% PEG300+water 4.6 mg/mL clear

PO 0.5% CMC-Na 52 mg/mL suspension

TG101209 99%+

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JAK3	JAK3, IC50:169 nM
JAK2	JAK2, IC50:6 nM
c-RET	RET, IC50:17 nM

TG101209 99%+

TG101209 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

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TG101209 纯度/质量文件产品仅供科研