JAK2/FLT3-IN-1

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JAK2/FLT3-IN-1 

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。

JAK2/FLT3-IN-1

JAK2/FLT3-IN-1 Chemical Structure

CAS No. : 2387765-27-5

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JAK2/FLT3-IN-1 的其他形式现货产品:

JAK2/FLT3-IN-1 TFA

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[1].

IC50 & Target[1]

JAK2

0.7 nM (IC50)

FLT3

4 nM (IC50)

JAK1

26 nM (IC50)

JAK3

39 nM (IC50)

体外研究
(In Vitro)

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

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

467.58

Formula

C25H34FN7O
CAS 号

2387765-27-5
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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

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
*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Yang T, et al. Discovery of Potent and Orally Effective Dual JAK2/FLT3 Inhibitors for the Treatment of AcuteMyelogenous Leukemia and Myeloproliferative Neoplasms. J Med Chem. 2019 Oct 31.

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