化合物 TG101209|T3065|TargetMol

TG101209
936091-14-4

￥348 2mg 起订

￥583 5mg 起订

￥995 10mg 起订

上海更新日期：2024-09-29

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 TG101209

英文名称：: TG101209

CAS号：: 936091-14-4

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99%

产品类别：: 抑制剂

货号：: T3065

Product Introduction

Bioactivity

Name	TG101209
Description	TG101209 is a selective JAK2 inhibitor with IC50 of 6 nM.
Cell Research	In brief, approximately 2 × 103 cells are plated into microtiterplate wells in 100 ml RPMI-1640 growth media with indicated concentrations of TG101209. The relative growth of cells is quantified at 24-hour intervals using Cell Proliferation Kit II (XTT) as per manufacturer's guidelines. After incubation, 20 mL of XTT is added to the wells and allowed to incubate for 4-6 hours. The colored formazan product is measured spectrophotometrically at 450 nm with correction at 650 nm, and IC50 values are determined using the GraphPad Prism 4.0 software. Data are subjected to a non-linear regression-fit analysis and IC50 values are determined as the concentration that inhibited proliferation by 50%. All experiments are done in triplicate and the results normalized to growth of untreated cells.(Only for Reference)
Kinase Assay	Cell-free Kinase Activity Assays: IC50 values for TG101209 are determined using a luminescence-based kinase assay with recombinant JAK2, VEGFR2/KDR, and JAK3 obtained from Upstate Cell Signaling Solutions. Kinase reactions are carried out in a buffer consisting of 40 mM Tris buffer (pH 7.4), 50 mM MgCl2, 800?M EGTA, 350?M Triton X-100, 2?M ?-mercaptoethanol, 100?M peptide substrate, and an appropriate amount of JAK2, VEGFR2/KDR or JAK3 such that the assay is linear over 60 minutes. The reaction is initiated by the addition of 10?L of ATP to a final concentration of 3 mM and terminated by the addition of Kinase-Glo reagent after 60 minutes. Luciferase activity is quantified using an Ultra 384 instrument set for luminosity measurements. IC50 values are derived from experimental data using the non-linear curve fitting capabilities of the GraphPad Prism 4.0 software. The single concentration inhibition data for a panel of 63 kinases is determined using the SelectScreen TM service.
In vitro	与安慰剂处理的动物相比,TG101209处理的动物体内循环肿瘤细胞负荷显著减少,呈剂量依赖性,在+11天时减少比例达到20%.100 mg/kg TG101209有效延长JAK2V617F诱发的患病动物的存活时间（10天）.
In vivo	TG101209抑制HCC2429和H460肺癌细胞中存活素,并降低STAT3的磷酸化作用。TG101209在表达人JAK2V617F的急性髓细胞性白血病细胞系中,诱导细胞周期阻滞和细胞凋亡,并抑制JAK2V617F,STAT5和STAT3的磷酸化。TG101209抑制表达JAK2V617F或MPLW515L突变体的Ba/F3细胞生长,IC50为B200 nM。TG101209抑制来自携带JAK2V617F或MPL515突变的原始祖细胞的造血集落的生长。TG101209明显减少STAT5磷酸化,而不影响STAT5蛋白质的总量。TG101209消除BCR-JAK2和STAT5的磷酸化,减少Bcl-xL表达,并引发转化的Ba/F3细胞凋亡。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 94 mg/mL (184.4 mM) Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble)
Keywords	Cluster of differentiation antigen 135 \| RET \| TG101209 \| Inhibitor \| Janus kinase \| TG-101209 \| CD135 \| Fms like tyrosine kinase 3 \| FLT3 \| Apoptosis \| TG 101209 \| JAK \| inhibit \| Autophagy
Inhibitors Related	Guanidine hydrochloride \| Naringin \| Taurine \| Gefitinib \| Hydroxychloroquine \| 5-Fluorouracil \| Curcumin \| Stavudine \| Tributyrin \| L-Ascorbic acid \| Paeonol \| Sodium 4-phenylbutyrate
Related Compound Libraries	Inhibitor Library \| Bioactive Compound Library \| Bioactive Compounds Library Max \| Anti-Pancreatic Cancer Compound Library \| Kinase Inhibitor Library \| Anti-Aging Compound Library \| Stem Cell Differentiation Compound Library \| Anti-Liver Cancer Compound Library \| Anti-Obesity Compound Library \| Tyrosine Kinase Inhibitor Library

TG101209|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

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