JAK2/FLT3-IN-1 (TFA) 是一种口服有效的双重JAK2/FLT3抑制剂，对 JAK2，FLT3，JAK1 和 JAK3 的IC50分别为 0.7 nM，4 nM，26 nM 和 39 nM。JAK2/FLT3-IN-1 (TFA) 具有抗癌活性。
| 生物活性 | JAK2/FLT3-IN-1 (TFA) is a potent and orally active dualJAK2/FLT3inhibitor withIC50values of 0.7 nM, 4 nM, 26 nM and 39 nM forJAK2,FLT3,JAK1andJAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity[1]. |
| IC50& Target | JAK1 26 nM (IC50) | JAK2 0.7 nM (IC50) | JAK3 39 nM (IC50) | FLT3 4 nM (IC50) |
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体外研究
(In Vitro) | JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) (TFA) down-regulates p-FLT3 in a dose-dependent manner[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) has a dose-dependent effect on the induction of apoptosis in the MV4-11 cells[1].
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) (TFA) strongly induces cell cycle arrest with a G1/G0 percentage of 85% at 100 nM in the MV4-11 cells[1].
Western Blot Analysis[1] | Cell Line: | MV4-11 and SET-2 cells | | Concentration: | 0.008, 0.04, 0.2, 1 μM | | Incubation Time: | For 2 hours | | Result: | Down-regulated p-FLT3 in a dose-dependent manner from 0.008 to 1 μM. |
Apoptosis Analysis[1] | Cell Line: | MV4-11 cells | | Concentration: | 5, 10, 50, 100 nM | | Incubation Time: | For 2 hours | | Result: | Had a dose-dependent effect on the induction of apoptosis in the MV4-11 cells. |
Cell Cycle Analysis[1] | Cell Line: | MV4-11 cells | | Concentration: | 5, 10, 50, 100 nM | | Incubation Time: | For 2 hours | | Result: | Induced cell cycle arrest with a G1/G0 percentage of 85% at 100 nM. |
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体内研究
(In Vivo) | JAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) (TFA) exhibits significant antitumor effects[1].
| Animal Model: | NOD/SCID mouse models[1] | | Dosage: | 30 and 60 mg/kg | | Administration: | Oral administration; daily; for 14 days | | Result: | Exhibited significant antitumor effects.
The tumor growth inhibitory rates (TGI) were respective 58% and 93% in the MV4-11-bearing mice model. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : 33.33 mg/mL(57.31 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.7194 mL | 8.5968 mL | 17.1937 mL | | 5 mM | 0.3439 mL | 1.7194 mL | 3.4387 mL | | 10 mM | 0.1719 mL | 0.8597 mL | 1.7194 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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