TG101209
| CAS号 | 936091-14-4 | 货号 | BCP02514 |
| 中文名 | TG101209 | ||
| 英文名 | TG101209 | ||
| 中文别名 | |||
| 英文别名 | TG 101209;TG-101209; | ||
| 分子式 | C26H35N7O2S | 分子量 | 509.67 |
| 生物活性 | 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 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. 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 triggered apoptosis of transformed Ba/F3 cells. | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway Wnt/Stem Cell Epigenetics | ||
| 靶 点 | Epigenetic Reader Domain FLT3 RET JAK | ||
结构式
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