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

TG101209 {[allProObj[0].p_purity_real_show]}

货号：A469558

TG101209是一种选择性的 JAK2 抑制剂，IC50 为 6 nM，同时抑制 Flt3 和 RET，IC50 分别为 25 nM 和 17 nM，对 JAK2 的选择性比 JAK3 高 30 倍，适用于癌症相关研究。

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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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 (2), Ki: 0.34 μM BRD4 (1), Ki: <0.085 μM						99%+
CPI-203	+++ BRD4, IC50: 37 nM						98+%
GSK1324726A	+++ BRD4, IC50: 22 nM BRD2, IC50: 31 nM						99%+
PFI-1	++ BRD4, IC50: 0.22 μM BRD2, IC50: 98 nM						98%
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (2), IC50: 33 nM BRD4 (1), IC50: 77 nM						98%
I-BET151	+ BRD4, IC50: 0.5 μM BRD3, IC50: 0.25 μM						98%
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						97%
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	++ BRD2, IC50: 0.29 μM BRD9, IC50: 0.122 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					98%
AZD5153 6-Hydroxy-2-naphthoic acid	++++ FL-BRD4, IC50: 5 nM						99%+
PLX51107	++++ BRD4 BD2, Kd: 1.7 nM BRD3 BD1, Kd: 2.1 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	++++ Brd3(BD2), Kd: 13 nM Brd2(BD2), Kd: 62 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-BD1, IC50: 5 nM BRD4-BD2, IC50: 41 nM						97%
A1874	✔						99%+
Y06036	++ BRD4 (1), Kd: 82 nM						99%+
Alobresib	✔					NF-κB	95%
ODM-207	✔						98%
GSK778	+++ BRD4-BD1, IC50: 143 nM BRD2-BD1, IC50: 75nM						97%
SRX3207	+ BRD42, IC50: 3070 nM BRD41, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD4_BD2, IC50: 214 nM BRD3_BD2, IC50: 98 nM						98%
GSK620	✔						97%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						98%
GSK2801		++ BAZ2A, Kd: 257 nM BAZ2B, Kd: 136 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		✔					98%
UNC926		+ L3MBTL1, Kd: 3.9 μM					99%
666-15		++ CREB, IC50: 81 nM					99%+
UNC6852		+ EED, IC50: 247 nM					98%
BAZ1A-IN-1		+ BAZ1A, Kd: 0.52 μM					99%+
PFI-4			++ BRPF1, IC50: 80 nM BRPF2, IC50: 7.9 μM				99%+
OF-1			++ BRPF2, Kd: 500 nM BRPF1B, Kd: 100 nM				99%+
GSK-5959			++ BRPF3, pIC50: 7.1 BRPF2, pIC50: 5.2				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF1, IC50: 48 nM BRPF3, IC50: 260 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			99%
I-CBP112					++ CBP, Kd: 151 nM p300, Kd: 167 nM		98+%
Histone Acetyltransferase Inhibitor II					+ p300, IC50: 5 μM		98%
C646					+ p300/CBP, Ki: 400 nM		99%+
Anacardic Acid					+ p300/CBP, IC50: 8.5 μM PCAF, IC50: 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%
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 wt, IC50: 1.3 nM RET V804M, IC50: 0.6 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				98%
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		95%
Peficitinib		✔				98%
Go6976		✔			FLT3	99%+
AZD-1480		++++ JAK2, IC50: 0.26 nM				99%+
Fedratinib		+++ JAK2, IC50: 3 nM JAK2 (V617F), IC50: 3 nM			RET,FLT3	99%+
WP1066		+ JAK2, IC50: 2.3 μM				98%
Curcumol		✔				98%
AZ960		++++ JAK2, Ki: 0.45 nM JAK2, IC50: <3 nM				97%
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	98%
BMS-911543		++++ JAK2, IC50: 1.1 nM	+ JAK3, IC50: 75 nM	++ TYK2, IC50: 66 nM		95%
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, IC50: 23 nM JAK2 (V617F), IC50: 19 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			98%
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	98%
Go6976	✔		99%+
Quizartinib	+++ FLT3 (WT), IC50: 4.2 nM FLT3 (ITD), IC50: 1.1 nM		98%
Gilteritinib	++++ FLT3, IC50: 0.29 nM		99%+
Amuvatinib	+ FLT3 (D835Y), IC50: 81 nM		99%+
Pacritinib	++ FLT3, IC50: 22 nM FLT3 (D835Y), IC50: 6 nM		97%
Dovitinib	++++ FLT3, IC50: 1 nM	c-Kit	99%+
Denfivontinib	++++ FLT3, IC50: 0.4 nM FLT3 (D835Y), 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 细胞实验

Cell Line MM1.S RPMI 8226 Caki-1 U266 SET-2V617F cells TEL-JAK2 T-ALL cells SET-2V617F cells HCC2429 CD34+ CML cells H460 Ba/F3-JAK2-V617F cells K562 cells BaF3-EPOR cells	Concentration	Treated Time	Description	References
MM1.S	5 µM	6, 24, 48 hours	Induction of apoptosis	Am J Hematol. 2010 Sep;85(9):675-86.
RPMI 8226	5 µM	6, 24, 48 hours	Induction of apoptosis	Am J Hematol. 2010 Sep;85(9):675-86.
Caki-1	6 nM	1 day	To validate the inhibitory effect of TG-101209 on BUB1B	EBioMedicine. 2022 Apr;78:103963.
U266	5 µM	48 hours	Preferential killing of CD45+ cells	Am J Hematol. 2010 Sep;85(9):675-86.
SET-2V617F cells	0.125–2 µM	48 hours	TG101209 induced dose-dependent apoptosis	Cell Rep. 2013 Nov 27;5(4):1047-59.
TEL-JAK2 T-ALL cells	0.125–4 µM	24 hours	To evaluate the killing effect of TG101209 on TEL-JAK2 T-ALL cells, the results showed that TG101209 induced dose-dependent apoptosis.	Cell Rep. 2013 Nov 27;5(4):1047-59.
SET-2V617F cells	0.125–2 µM	24 hours	To evaluate the killing effect of TG101209 on SET-2V617F cells, the results showed that TG101209 induced dose-dependent apoptosis.	Cell Rep. 2013 Nov 27;5(4):1047-59.
HCC2429	1 µM	24-48 hours	Inhibited STAT3 phosphorylation and survivin expression, sensitized cells to radiation	J Thorac Oncol. 2011 Apr;6(4):699-706.
CD34+ CML cells	100 nM	3 days	To evaluate the growth inhibitory effect of TG101209 on CD34+ CML cells, results showed that TG101209 significantly inhibited the growth of CD34+ CML cells.	J Natl Cancer Inst. 2013 Mar 20;105(6):405-23.
H460	3 µM	48 hours	Inhibited STAT3 phosphorylation and survivin expression, sensitized cells to radiation	J Thorac Oncol. 2011 Apr;6(4):699-706.
Ba/F3-JAK2-V617F cells	10 nM, 15 nM, 20 nM	48 hours	Induced apoptosis in Ba/F3-JAK2-V617F cells	Clin Cancer Res. 2011 Dec 1;17(23):7347-58.
K562 cells	0.5 µM	48 hours	To evaluate the growth inhibitory effect of TG101209 on K562 cells, results showed that TG101209 significantly inhibited the growth of K562 cells.	J Natl Cancer Inst. 2013 Mar 20;105(6):405-23.
BaF3-EPOR cells	0.6 µM		TG101209 mildly inhibited colony formation of BaF3-EPOR cells plated on methylcellulose containing a sub-saturating EPO concentration.	Nat Med. 2011 Jun 19;17(7):845-53.

Cell Line

Concentration

Treated Time

Description

References

MM1.S

5 µM

6, 24, 48 hours

Induction of apoptosis

Am J Hematol. 2010 Sep;85(9):675-86.

RPMI 8226

5 µM

6, 24, 48 hours

Induction of apoptosis

Am J Hematol. 2010 Sep;85(9):675-86.

Caki-1

6 nM

1 day

To validate the inhibitory effect of TG-101209 on BUB1B

EBioMedicine. 2022 Apr;78:103963.

U266

5 µM

48 hours

Preferential killing of CD45+ cells

Am J Hematol. 2010 Sep;85(9):675-86.

SET-2V617F cells

0.125–2 µM

48 hours

TG101209 induced dose-dependent apoptosis

Cell Rep. 2013 Nov 27;5(4):1047-59.

TEL-JAK2 T-ALL cells

0.125–4 µM

24 hours

To evaluate the killing effect of TG101209 on TEL-JAK2 T-ALL cells, the results showed that TG101209 induced dose-dependent apoptosis.

Cell Rep. 2013 Nov 27;5(4):1047-59.

SET-2V617F cells

0.125–2 µM

24 hours

To evaluate the killing effect of TG101209 on SET-2V617F cells, the results showed that TG101209 induced dose-dependent apoptosis.

Cell Rep. 2013 Nov 27;5(4):1047-59.

HCC2429

1 µM

24-48 hours

Inhibited STAT3 phosphorylation and survivin expression, sensitized cells to radiation

J Thorac Oncol. 2011 Apr;6(4):699-706.

CD34+ CML cells

100 nM

3 days

To evaluate the growth inhibitory effect of TG101209 on CD34+ CML cells, results showed that TG101209 significantly inhibited the growth of CD34+ CML cells.

J Natl Cancer Inst. 2013 Mar 20;105(6):405-23.

H460

3 µM

48 hours

Inhibited STAT3 phosphorylation and survivin expression, sensitized cells to radiation

J Thorac Oncol. 2011 Apr;6(4):699-706.

Ba/F3-JAK2-V617F cells

10 nM, 15 nM, 20 nM

48 hours

Induced apoptosis in Ba/F3-JAK2-V617F cells

Clin Cancer Res. 2011 Dec 1;17(23):7347-58.

K562 cells

0.5 µM

48 hours

To evaluate the growth inhibitory effect of TG101209 on K562 cells, results showed that TG101209 significantly inhibited the growth of K562 cells.

J Natl Cancer Inst. 2013 Mar 20;105(6):405-23.

BaF3-EPOR cells

0.6 µM

TG101209 mildly inhibited colony formation of BaF3-EPOR cells plated on methylcellulose containing a sub-saturating EPO concentration.

Nat Med. 2011 Jun 19;17(7):845-53.

TG101209 动物实验

Species Nude mice Mice Mice Mice Mice Mice	Animal Model Lung cancer xenograft model AE9a leukemia mouse model TEL-JAK2 T-ALL model TEL-JAK2 T-ALL model VhlR200W/R200W knock-in mice NOD/SCID–IL2Rγ-deficient mice	Administration	Dosage	Frequency	Description	References
Nude mice	Lung cancer xenograft model	Oral	100 mg/kg	Twice daily for 7 consecutive days	Combination of TG101209 and radiation significantly extended tumor growth delay, increased apoptosis, and reduced tumor proliferation and vascular density	J Thorac Oncol. 2011 Apr;6(4):699-706.
Mice	AE9a leukemia mouse model	Oral	100 mg/kg	Twice daily for two weeks	TG101209 effectively reduced tumor burden in AE9a leukemia mice and significantly prolonged survival.	Leukemia. 2013 Dec;27(12):2272-9
Mice	TEL-JAK2 T-ALL model	Oral	100 mg/kg bid	Twice daily for 4 days	To evaluate the therapeutic effect of TG101209 on TEL-JAK2 T-ALL model mice, the results showed that TG101209 significantly reduced tumor cells in peripheral blood and spleen and prolonged the survival of mice.	Cell Rep. 2013 Nov 27;5(4):1047-59.
Mice	TEL-JAK2 T-ALL model	Oral	100 mg/kg bid	Twice daily for 4 days	TG101209 significantly reduced tumor cells in peripheral blood and spleen and prolonged the survival of mice	Cell Rep. 2013 Nov 27;5(4):1047-59.
Mice	VhlR200W/R200W knock-in mice	Oral gavage	100mg/kg	Twice daily for 5 weeks	TG101209 treatment reversed the disease phenotype in vhlR200W/R200W knock-in mice, reducing hematocrit (Hct) levels and decreasing the number of megakaryocytes in the spleen.	Nat Med. 2011 Jun 19;17(7):845-53.
Mice	NOD/SCID–IL2Rγ-deficient mice	Oral	60 mg/kg	Twice a day for 2 weeks	To evaluate the effect of combined treatment with TG101209 and imatinib on the survival of leukemic mice, results showed that the combination treatment significantly prolonged the survival of mice.	J Natl Cancer Inst. 2013 Mar 20;105(6):405-23.

Species

Nude mice Mice Mice Mice Mice Mice

Animal Model

Lung cancer xenograft model AE9a leukemia mouse model TEL-JAK2 T-ALL model TEL-JAK2 T-ALL model VhlR200W/R200W knock-in mice NOD/SCID–IL2Rγ-deficient mice

Administration

Dosage

Frequency

Description

References

Nude mice

Lung cancer xenograft model

Oral

100 mg/kg

Twice daily for 7 consecutive days

Combination of TG101209 and radiation significantly extended tumor growth delay, increased apoptosis, and reduced tumor proliferation and vascular density

J Thorac Oncol. 2011 Apr;6(4):699-706.

Mice

AE9a leukemia mouse model

Oral

100 mg/kg

Twice daily for two weeks

TG101209 effectively reduced tumor burden in AE9a leukemia mice and significantly prolonged survival.

Leukemia. 2013 Dec;27(12):2272-9

Mice

TEL-JAK2 T-ALL model

Oral

100 mg/kg bid

Twice daily for 4 days

To evaluate the therapeutic effect of TG101209 on TEL-JAK2 T-ALL model mice, the results showed that TG101209 significantly reduced tumor cells in peripheral blood and spleen and prolonged the survival of mice.

Cell Rep. 2013 Nov 27;5(4):1047-59.

Mice

TEL-JAK2 T-ALL model

Oral

100 mg/kg bid

Twice daily for 4 days

TG101209 significantly reduced tumor cells in peripheral blood and spleen and prolonged the survival of mice

Cell Rep. 2013 Nov 27;5(4):1047-59.

Mice

VhlR200W/R200W knock-in mice

Oral gavage

100mg/kg

Twice daily for 5 weeks

TG101209 treatment reversed the disease phenotype in vhlR200W/R200W knock-in mice, reducing hematocrit (Hct) levels and decreasing the number of megakaryocytes in the spleen.

Nat Med. 2011 Jun 19;17(7):845-53.

Mice

NOD/SCID–IL2Rγ-deficient mice

Oral

60 mg/kg

Twice a day for 2 weeks

To evaluate the effect of combined treatment with TG101209 and imatinib on the survival of leukemic mice, results showed that the combination treatment significantly prolonged the survival of mice.

J Natl Cancer Inst. 2013 Mar 20;105(6):405-23.

TG101209 参考文献

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	509.67
SMILES Code	O=S(C1=CC=CC(NC2=NC(NC3=CC=C(N4CCN(C)CC4)C=C3)=NC=C2C)=C1)(NC(C)(C)C)=O
MDL No.	MFCD15528085

别名
运输	蓝冰
InChI Key	JVDOKQYTTYUYDV-UHFFFAOYSA-N
Pubchem ID	16722832

存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C

溶解方案

细胞实验：

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：请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用；以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

方案二

TG101209 {[allProObj[0].p_purity_real_show]}

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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].

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

TG101209 {[allProObj[0].p_purity_real_show]}

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

TG101209 质控信息

TG101209 生物活性

TG101209 细胞实验

TG101209 动物实验

TG101209 参考文献

TG101209 实验方案

TG101209 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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TG101209 纯度/质量文件产品仅供科研