Fedratinib hydrochloride hydrate TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate|cas:1374744-69-0|西域试剂

Fedratinib hydrochloride hydrate TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate,99.86%

产品编号：Bellancom-10409A| CAS NO：1374744-69-0| 分子式：C₂₇H₄₀Cl₂N₆O₄S| 分子量：615.62

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货号	价格	库存与货期
Bellancom-10409A	￥500.00	杭州北京（现货）
Bellancom-10409A	￥700.00	杭州北京（现货）
Bellancom-10409A	￥1500.00	杭州北京（现货）
Bellancom-10409A	￥2500.00	杭州北京（现货）
Bellancom-10409A	￥5500.00	杭州北京（现货）

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Fedratinib hydrochloride hydrate TG-101348 hydrochloride hydrate; SAR 302503 hydrochloride hydrate

产品介绍

Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) 是一种有效的，选择性的，ATP 竞争性和具有口服活性的 JAK2 抑制剂，对于 JAK2 和 JAK2V617F 激酶的 IC₅₀ 均为 3 nM。Fedratinib hydrochloride hydrate 对 JAK2 的选择性分别比 JAK1 和 JAK3 高 35 倍和 334 倍。Fedratinib hydrochloride hydrate 可诱导癌细胞凋亡 (apoptosis)，并可用于骨髓增生性疾病的研究。

生物活性

Fedratinib hydrochloride hydrate (TG-101348 hydrochloride hydrate) is a potent, selective, ATP-competitive and orally active JAK2 inhibitor with IC₅₀s of 3 nM for both JAK2 and JAK2V617F kinase. Fedratinib hydrochloride hydrate shows 35- and 334-fold selectivity over JAK1 and JAK3, respectively. Fedratinib hydrochloride hydrate induces cancer cell apoptosis and has the potential for myeloproliferative disorders research.

体外研究

Fedratinib (TG101348) inhibits proliferation of a human erythroblast leukemia (HEL) cell line that harbors the JAK2V617F mutation, as well as a murine pro-B cell line expressing human JAK2V617F (Ba/F3 JAK2V617F), with an IC₅₀ value of approximately 300 nM for either line. Proliferation of parental Ba/F3 cells was inhibited to a comparable level, with an IC₅₀ value of ∼420 nM.
Exposure of these cells to Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) reduces STAT5 phosphorylation at concentrations that parallel the concentrations required to inhibit cell proliferation.
Fedratinib (TG101348) (0.1 μM, 0.3 μM, 1 μM, 3 μM, and 10 μM) induces apoptosis in both HEL and Ba/F3 JAK2V617F cells in a dose-dependent manner.

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

体内研究

Fedratinib (TG101348; 60-120 mg/kg; oral gavage; twice daily; for 42 days; C57Bl/6 mice) trewatment shows a dose-dependent reduction in polycythemia and a marked dose-dependent reduction in splenomegaly of treated animals.

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

Animal Model:	C57Bl/6 mice induced by the JAK2V617F mutation
Dosage:	60 mg/kg, 120 mg/kg
Administration:	Oral gavage; twice daily; for 42 days
Result:	Showed a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis.

体内研究

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

Animal Model:	C57Bl/6 mice induced by the JAK2V617F mutation
Dosage:	60 mg/kg, 120 mg/kg
Administration:	Oral gavage; twice daily; for 42 days
Result:	Showed a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (203.05 mM; Need ultrasonic)

H₂O : 100 mg/mL (162.44 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6244 mL	8.1219 mL	16.2438 mL
5 mM	0.3249 mL	1.6244 mL	3.2488 mL
10 mM	0.1624 mL	0.8122 mL	1.6244 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。

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 (3.38 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.38 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 (3.38 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.38 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 (3.38 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.38 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。