Tandutinib hydrochloride MLN518 hydrochloride; CT53518 hydrochloride|cas:2438900-70-8|西域试剂

Tandutinib hydrochloride MLN518 hydrochloride; CT53518 hydrochloride,99.78%

产品编号：Bellancom-10202A| CAS NO：2438900-70-8| 分子式：C₃₁H₄₃ClN₆O₄| 分子量：599.16

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-10202A		￥550.00	杭州北京（现货）
Bellancom-10202A		￥884.00	杭州北京（现货）

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Tandutinib hydrochloride MLN518 hydrochloride; CT53518 hydrochloride

产品介绍

Tandutinib hydrochloride (MLN518 hydrochloride) 是一种有效和选择性的 FLT3 的抑制剂，其 IC₅₀ 为 0.22 μM，并且还抑制 c-Kit 和 PDGFR，其 IC₅₀ 分别为 0.17 μM 和 0.20 μM。Tandutinib hydrochloride 可用于急性骨髓性白血病，并具有穿越血脑屏障的能力。

生物活性

Tandutinib hydrochloride (MLN518 hydrochloride) is a potent and selective inhibitor of the FLT3 with an IC₅₀ of 0.22 μM, and also inhibits c-Kit and PDGFR with IC₅₀s of 0.17 μM and 0.20 μM, respectively. Tandutinib hydrochloride can be used for acute myelogenous leukemia (AML). Tandutinib hydrochloride has the ability to cross the blood-brain barrier.

体外研究

Tandutinib (0-3 μM; 30 minutes; Ba/F3 cells) treatment inhibits IL-3-independent cell growth and FLT3-ITD autophosphorylation with an IC₅₀ of 10-100 nM in Ba/F3 cells expressing different FLT3-ITD mutants.
Tandutinib (1 μM; 24-96 hours; Molm-14 and THP-1 AML cells) treatment induces apoptosis in FLT3-ITD-positive AML cells.
In human FLT3-ITD-positive AML cell lines, Tandutinib inhibits FLT3-ITD phosphorylation (IC₅₀ of ~30 nM). As with Erk2, a constitutively high level of Akt phosphorylation is readily detected and is efficiently blocked by pretreatment of the Molm-14 cells with 100-300 nM Tandutinib.
Tandutinib inhibits cell proliferation of the FLT3-ITD-positive Molm-13 and Molm-14 with an IC₅₀ of 10 nM. And signaling through the MAP kinase and PI3 kinase pathways.

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

Apoptosis Analysis

Cell Line:	Molm-14 and THP-1 AML cells
Concentration:	1 μM
Incubation Time:	24 hours, 48 hours, 72 hours, 96 hours
Result:	Induced apoptosis in FLT3-ITD-positive AML cells.

Western Blot Analysis

Cell Line:	Ba/F3 cells
Concentration:	0 μM, 0.003 μM, 0.01 μM, 0.03 μM, 0.1 μM, 1 μM and 3 μM
Incubation Time:	30 minutes
Result:	In Ba/F3 cells expressing different FLT3-ITD mutants, inhibited IL-3-independent cell growth and FLT3-ITD autophosphorylation.

体内研究
(In Vivo)

Tandutinib (60 mg/kg; oral gavage; daily; for 35 days; athymic nude mice) treatment causes a statistically significant increase in survival that was extended on average by 20 days.

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

Animal Model:	Athymic nude mice injected with Ba/F3 cells
Dosage:	60 mg/kg
Administration:	Oral gavage; daily; for 35 days
Result:	Caused a statistically significant increase in survival that was extended on average by 20 days.

体内研究

Tandutinib (60 mg/kg; oral gavage; daily; for 35 days; athymic nude mice) treatment causes a statistically significant increase in survival that was extended on average by 20 days.

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

Animal Model:	Athymic nude mice injected with Ba/F3 cells
Dosage:	60 mg/kg
Administration:	Oral gavage; daily; for 35 days
Result:	Caused a statistically significant increase in survival that was extended on average by 20 days.

体内研究

Tandutinib (60 mg/kg; oral gavage; daily; for 35 days; athymic nude mice) treatment causes a statistically significant increase in survival that was extended on average by 20 days.

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

Animal Model:	Athymic nude mice injected with Ba/F3 cells
Dosage:	60 mg/kg
Administration:	Oral gavage; daily; for 35 days
Result:	Caused a statistically significant increase in survival that was extended on average by 20 days.

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (166.90 mM)

H₂O : 100 mg/mL (166.90 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6690 mL	8.3450 mL	16.6900 mL
5 mM	0.3338 mL	1.6690 mL	3.3380 mL
10 mM	0.1669 mL	0.8345 mL	1.6690 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： PBS
Solubility: 100 mg/mL (166.90 mM); Clear solution; Need ultrasonic
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.17 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.17 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.17 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.17 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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