JAK2-IN-7|cas:2593402-36-7|西域试剂

JAK2-IN-7,99.42%

产品编号：Bellancom-131906| CAS NO：2593402-36-7| 分子式：C₂₆H₃₃N₇O| 分子量：459.59

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-131906	￥4500.00	杭州北京（现货）
Bellancom-131906	￥8000.00	杭州北京（现货）
Bellancom-131906	￥16500.00	杭州北京（现货）
Bellancom-131906	￥25500.00	杭州北京（现货）
Bellancom-131906	￥38000.00	杭州北京（现货）

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JAK2-IN-7

产品介绍

JAK2-IN-7 是一种选择性 JAK2 抑制剂，对 JAK2，SET-2 和 Ba/F3^V617F细胞的 IC₅₀ 为 3、11.7 和 41 nM。 JAK2-IN-7 的选择性是 JAK1, JAK3，FLT3 的 14 倍以上。JAK2-IN-7 刺激细胞周期停滞在 G0/G1 期，并诱导肿瘤细胞凋亡 (apoptosis)。抗肿瘤活性。

生物活性

JAK2-IN-7 is a selective JAK2 inhibitor with IC₅₀s of 3, 11.7, and 41 nM for JAK2, SET-2, and Ba/F3^V617F cells, respectively. JAK2-IN-7 possesses >14-fold selectivity over JAK1, JAK3, FLT3. JAK2-IN-7 stimulates cell cycle arrest in the G0/G1 phase and induces tumor cellapoptosis. Antitumor activities.

体外研究

JAK2-IN-7 (compound 13ac) (0-1000 nM; 2 hours) inhibits JAK2 and STAT5 phosphorylation in a dose-dependent manner in SET-2 and Ba/F3-JAK2^V617F cells.
JAK2-IN-7 (10-160 nM; 24 hours) induces cell arrest in the G0/G1 phase.
JAK2-IN-7 (0.05-1.6 μM; 2 hours) induces apoptosis in SET-2 cells.

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

Cell Cycle Analysis

Cell Line:	SET-2 cells
Concentration:	10-160 nM
Incubation Time:	24 hours
Result:	Induced cell arrest in the G0/G1 phase in a concentration-dependent manner.

Apoptosis Analysis

Cell Line:	SET-2 cells
Concentration:	0.05-1.6 μM
Incubation Time:	2 hours
Result:	Induced apoptosis in SET-2 cells.

体内研究
(In Vivo)

JAK2-IN-7 (15-60 mg/kg; p.o.; daily for 16 days) shows potent in vivo antitumor efficacy with 82.3% tumor growth inhibition in the SET-2 xenograft model.
JAK2-IN-7 (30-60 mg/kg; p.o.; q.d. for 16 day) significantly ameliorates the disease symptoms in a Ba/F3-JAK2V617F allograft model, with 77.1% normalization of spleen weight, which was more potent than Ruxolitinib.

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

Animal Model:	SET-2 cell-inoculated xenograft NOD/SCID mouse model
Dosage:	15, 30, and 60 mg/kg
Administration:	Orally daily for 16 days
Result:	Exhibited a significant tumor growth inhibition of 82.3% without obvious weight change.

体内研究

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

Animal Model:	SET-2 cell-inoculated xenograft NOD/SCID mouse model
Dosage:	15, 30, and 60 mg/kg
Administration:	Orally daily for 16 days
Result:	Exhibited a significant tumor growth inhibition of 82.3% without obvious weight change.

体内研究

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

Animal Model:	SET-2 cell-inoculated xenograft NOD/SCID mouse model
Dosage:	15, 30, and 60 mg/kg
Administration:	Orally daily for 16 days
Result:	Exhibited a significant tumor growth inhibition of 82.3% without obvious weight change.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (543.96 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1759 mL	10.8793 mL	21.7585 mL
5 mM	0.4352 mL	2.1759 mL	4.3517 mL
10 mM	0.2176 mL	1.0879 mL	2.1759 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 (4.53 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.53 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 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 (4.53 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.53 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.53 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.53 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
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玉米油中，混合均匀。