PLX647
| CAS号 | 873786-09-5 | 货号 | BCP15182 |
| 中文名 | PLX647 | ||
| 英文名 | PLX647 | ||
| 中文别名 | |||
| 英文别名 | PLX-647;PLX 647; | ||
| 分子式 | C21H17F3N4 | 分子量 | 382.38 |
| 生物活性 | in vitro: PLX647 was tested against a panel of 400 kinases at a concentration of 1 μM, 35-fold above its FMS enzymatic IC50 and 60-fold above its KIT enzymatic IC50. In addition to FMS and KIT, the activities of only nine kinases were inhibited by more than 50%. PLX647 potently inhibits the growth of FLT3–ITD-expressing MV4-11 cells (IC50 = 0.11 μM) but not OCI-AML5 (IC50 = 1.6 μM), which express wild-type FLT3. PLX647 displayed minimal inhibition of the proliferation of Ba/F3 cells expressing BCR–KDR (IC50 = 5 μM) . in vivo: PLX647 (40 mg/kg) was dosed orally 4.25 h before LPS injection. Treatment with PLX647 reduced serum TNF-α levels by 85% compared with the vehicle control. In the same experiment, the positive control dexamethasone (0.5 mg/kg, PO) lowered the TNF-α levels by 96%. Treatment with 40 mg/kg PLX647 also resulted in significant inhibition of IL-6 release (75%), with similar potency to dexamethasone (70%) . In the UUO kidneys, treatment with PLX647 [40 mg/kg twice daily ( | ||
| 信号通路 | Angiogenesis/Protein Tyrosine Kinase | ||
| 靶 点 | c Kit cFMS | ||
结构式
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