JAK2/FLT3-IN-1|cas:2387765-27-5|西域试剂

JAK2/FLT3-IN-1,99.79%

产品编号：Bellancom-130247| CAS NO：2387765-27-5| 分子式：C₂₅H₃₄FN₇O| 分子量：467.58

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

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JAK2/FLT3-IN-1

产品介绍

JAK2/FLT3-IN-1 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 具有抗癌活性。

生物活性

JAK2/FLT3-IN-1 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 has anti-cancer activity.

体外研究

JAK2/FLT3-IN-1 (0.008-1 μM; for 2 hours) down-regulates p-FLT3 in a dose-dependent manner.
JAK2/FLT3-IN-1 (5-100 nM; for 2 hours) 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) 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) 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) 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) 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:

DMSO : 20.83 mg/mL (44.55 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1387 mL	10.6934 mL	21.3867 mL
5 mM	0.4277 mL	2.1387 mL	4.2773 mL
10 mM	0.2139 mL	1.0693 mL	2.1387 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。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 2.08 mg/mL (4.45 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.45 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (4.45 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.45 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明