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TG101209
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
TG101209图片
CAS NO:936091-14-4
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议
1g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)509.67
FormulaC26H35N7O2S
CAS No.936091-14-4
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 102 mg/mL (200.12 mM)
Water:<1 mg/mL (slightly soluble or insoluble)
Ethanol: <1 mg/mL (slightly soluble or insoluble)
Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 12mg/mL
Synonyms/Chemical NameTG101209; TG-101209; TG 101209; N-tert-butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesulfonamide
实验参考方法
In VitroTG101209 is an orally bioavailable, small molecule, ATP-competitive inhibitor towards several tyrosine kinases. TG101209 inhibits growth of Ba/F3 cells expressing JAK2V617F or MPLW515L mutations with an IC50 of B200 nM. In a human JAK2V617F-expressing acute myeloid leukemia cell line, TG101209 inducs cell cycle arrest and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5 and STAT3
In Vivo100 mg/kg of TG101209 effectively prolongs the survival in JAK2V617F-induced disease (10 days). Compared with placebo-treated animals, TG101209-treated animals exhibit statistically significant, dose-dependent reduction in the circulating tumor cell burden at day +11 to 20%.
Animal modelBa/F3-V617F-GFP cells are injected into immunodeficient SCID mice to induce a rapidly fatal, fully penetrant hematopoietic disease.
Formulation & DosageTG101209 is dissolved in DMSO; 100 mg/kg; oral gavage
References[1] Pardanani A, et al, Leukemia, 2007, 21(8), 1658-1668.
生物活性

Mechanism of action of TG101209. Am J Hematol. 2010 Sep;85(9):675-86.

Preferential killing of CD45+ cells by TG101209. Am J Hematol. 2010 Sep;85(9):675-86.

TG101209 synergizes with PI3K inhibitor LY294002 in killing myeloma cells. Am J Hematol. 2010 Sep;85(9):675-86.