TG101209
目录号: PL10970 纯度: ≥99%

TG101209 是一种选择性的,有效的 JAK2 抑制剂,IC50 值为 6 nM;同时能抑制 Flt3,和 RET 的活性,IC50 值分别为 25 nM 和 17 nM。

CAS No. :936091-14-4
商品编号 规格 价格 会员价 是否有货 数量
PL10970-5mg 5mg ¥865.45 请登录
PL10970-10mg 10mg ¥1483.64 请登录
PL10970-50mg 50mg ¥3338.18 请登录
PL10970-100mg 100mg ¥5996.36 请登录
PL10970-200mg 200mg 询价 询价
PL10970-500mg 500mg 询价 询价
PL10970-10mM*1mLinDMSO 10mM*1mLinDMSO ¥970.55 请登录
Medlife所售产品仅用于科学研究(非临床研究),非药品不可食用,不可用于人体或动物的临床诊断和治疗,我们不为个人提供产品及服务。产品COA等资料,可至下方“质量控制”中下载。
中文名称
TG101209
中文别名
N-(1,1-二甲基乙基)-3-[[5-甲基-2-[[4-(4-甲基-1-哌嗪基)苯基]氨基]-4-嘧啶基]氨基]苯磺酰胺;N-(1,1-二甲基乙基)-3-[[5-甲基-2-[[4-(4-甲基-1-哌嗪)苯基]氨基]-4-嘧啶]氨基]苯磺酰胺;TG101209 抑制剂
英文名称
TG101209
英文别名
N-(tert-Butyl)-3-((5-methyl-2-((4-(4-methylpiperazin-1-yl)phenyl)amino)pyrimidin-4-yl)amino)benzenesulfonamide;TG101209;N-(1,1-DIMETHYLETHYL)-3-[[5-METHYL-2-[[4-(4-METHYL-1-PIPERAZINYL)PHENYL]AMINO]-4-PYRIMIDINYL]AMINO]BENZENESULFONAMIDE;N-tert-butyl-3-[[5-methyl-2-[4-(4-methylpiperazin-1-yl)anilino]pyrimidin-4-yl]amino]benzenesulfonamide;TG-101209;TG 101209;N-tert-butyl-3-(5-methyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-ylamino)benzenesulfonamide;N-tert-butyl-3-[(5-methyl-2-{[4-(4-methylpiperazin-1-yl)phenyl]amino}pyrimidin-4-yl)amino]benzenesulfonamide;C26H35N7O2S;N-(1,1-;N-(1,1-Dimethylethyl)-3-[[5-methyl-2-[[4-(4-methyl-1-piperazinyl)phenyl]amino]-4-pyrimidinyl]amino]benzenesulfonamide (ACI);SAR 317461
Cas No.
936091-14-4
分子式
C26H35N7O2S
分子量
509.67
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
TG101209 是一种选择性的,有效的 JAK2 抑制剂,IC50 值为 6 nM;同时能抑制 Flt3,和 RET 的活性,IC50 值分别为 25 nM 和 17 nM。
生物活性
TG101209 is a selective JAK2 inhibitor with IC 50 of 6 nM, less potent to Flt3 and RET with IC 50 of 25 nM and 17 nM, appr 30-fold selective for JAK2 than JAK3, and sensitive to JAK2V617F and MPLW515L/K mutations.
性状
Solid
IC50 & Target[1][2]
JAK2 6 nM (IC50) JAK3 169 nM (IC50
体外研究(In Vitro)
TG101209 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 200 nM. In a human JAK2V617F-expressing acute myeloid leukemia cell line, TG101209 induces cell cycle arrest and apoptosis, and inhibits phosphorylation of JAK2V617F, STAT5 and STAT3. TG101209 suppresses growth of hematopoietic colonies from primary progenitor cells harboring JAK2V617F or MPL515 mutations. TG101209 significantly reduces STAT5 phosphorylation without affecting the total amount of STAT5 protein. TG101209 inhibits survivin and reduces phosphorylation of STAT3 in HCC2429 and H460 lung cancer cells. TG101209 results in radio sensitization of HCC2429 and H460 lung cancer cells in vitro. A recent study indicates TG101209 abrogates BCR-JAK2 and STAT5
体内研究(In Vivo)
TG101209 (100 mg/kg) 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%. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Pardanani A, 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.
[2]. Ma AC, 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.
溶解度数据
In Vitro: DMSO : ≥ 50 mg/mL (98.10 mM)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2