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 dualJAK2/FLT3inhibitor withIC50values of 0.7 nM, 4 nM, 26 nM and 39 nM forJAK2,FLT3,JAK1andJAK3, 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) |
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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].
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) 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 | 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℃) 配制储备液 | 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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