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TG101209

CAS No. : 936091-14-4

MCE 站：TG101209

产品活性：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。

研究领域：Protein Tyrosine Kinase/RTK  |  JAK/STAT Signaling  |  Epigenetics  |  Stem Cell/Wnt  |  Autophagy  |  Apoptosis

作用靶点：FLT3  |  JAK  |  RET  |  Autophagy  |  Apoptosis

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 phosphorylation, decreases Bcl-xL expression and triggers apoptosis of transformed Ba/F3 cells.

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%.

相关产品：Bioactive Compound Library Plus  |  Apoptosis Compound Library  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Protein Tyrosine Kinase Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  MG-132  |  LY294002  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Paclitaxel  |  Y-27632 dihydrochloride  |  Acetylcysteine  |  Angiotensin II human  |  SP600125  |  5-Fluorouracil  |  Staurosporine  |  Bortezomib  |  Tamoxifen  |  2-Deoxy-D-glucose  |  Gemcitabine  |  Verteporfin  |  Decitabine  |  Actinomycin D  |  Temozolomide  |  BAY 11-7082  |  Etoposide  |  Mitomycin C  |  CCCP  |  DAPT  |  Rotenone  |  Etomoxir  |  Stattic  |  Docetaxel  |  Fulvestrant

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