| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| T409127-1ml |
1ml |
现货  |
|
| 英文别名 | N-tert-butyl-3-(5-methyl-2-(4-(4-methylpiperazin-1-yl)phenylamino)pyrimidin-4-ylamino)benzenesulfonamide |
|---|---|
| 规格或纯度 | 10mM in DMSO |
| 英文名称 | TG101209 |
| 生化机理 | TG101209 是一种选择性 JAK2 抑制剂，IC50 为 6 nM，对 Flt3 和 RET（c-RET）的作用较弱，在无细胞实验中的 IC50 分别为 25 nM 和 17 nM，对 JAK2 的选择性约为 JAK3 的 30 倍，对 JAK2V617F 和 MPLW515L/K 突变敏感。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 产品介绍 |
TG101209是JAK2选择性抑制剂，IC50为6 nM，对Flt3和RET的IC50为25 nM和17 nM，比对JAK3的抑制性高30倍，对JAK2V617F和MPLW515L/K突变型敏感，还能抑制BRD4，IC50为130 nM。An inhibitor of JAK2, Flt-3, Ret, and JAK3 Information TG101209 is a selectiveJAK2inhibitor withIC50of 6 nM, less potent to Flt3 and RET (c-RET) withIC50of 25 nM and 17 nM in cell-free assays, ~30-fold selective for JAK2 than JAK3, sensitive to JAK2V617F and MPLW515L/K mutations. 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. In vivo 100 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%. cell lines： Concentrations：4.6-38 400 nM Incubation Time：28-30 hours Powder Purity:≥96% |
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CC1=CN=C(N=C1NC2=CC(=CC=C2)S(=O)(=O)NC(C)(C)C)NC3=CC=C(C=C3)N4CCN(CC4)C |
| PubChem CID | 16722832 |
| 分子量 | 509.67 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 44 mg/mL (197.98 mM); Ethanol: 7 mg/mL (31.49 mM); Water: Insoluble; |
|---|
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