JAK2/FLT3-IN-1 TFA|西域试剂

JAK2/FLT3-IN-1 TFA,99.77%

产品编号：Bellancom-130247A| 分子式：C₂₇H₃₅F₄N₇O₃| 分子量：581.61

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-130247A		￥7500.00	杭州北京（现货）
Bellancom-130247A		￥12500.00	杭州北京（现货）

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JAK2/FLT3-IN-1 TFA

产品介绍

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 dual JAK2/FLT3 inhibitor with IC₅₀ values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 (TFA) has anti-cancer activity.

体外研究

JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) (TFA) down-regulates p-FLT3 in a dose-dependent manner.
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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis

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

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

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD/SCID mouse models
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.

体内研究

JAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) (TFA) exhibits significant antitumor effects.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD/SCID mouse models
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.

体内研究

JAK2/FLT3-IN-1 (30 and 60 mg/kg/day; p.o.; for 14 days) (TFA) exhibits significant antitumor effects.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	NOD/SCID mouse models
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.

性状

Solid

溶解性数据

In Vitro:

H₂O : 33.33 mg/mL (57.31 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

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)

参考文献