VTP50469|cas:2169916-18-9|西域试剂

VTP50469,99.94%

产品编号：Bellancom-114162| CAS NO：2169916-18-9| 分子式：C₃₂H₄₇FN₆O₄S| 分子量：630.82

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货号	价格	库存与货期
Bellancom-114162	￥3400.00	杭州北京（现货）
Bellancom-114162	￥5800.00	杭州北京（现货）
Bellancom-114162	￥0.00	杭州北京（现货）
Bellancom-114162	￥0.00	杭州北京（现货）

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VTP50469

产品介绍

VTP50469 是一种有效的，高选择性和口服活性的 Menin-MLL 相互作用抑制剂，K_i为 104 pM。VTP50469 具有高效的抗白血病活性。

生物活性

VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a K_i of 104 pM. VTP50469 has potently anti-leukemia activity.

体外研究

VTP50469 more potently and rapidly inhibits cell proliferation in a concentration-dependent manner in MLL-r cell lines carrying (MOLM13 (IC₅₀ of 13 nM), THP1 (IC₅₀ of 37 nM), NOMO1 (IC₅₀ of 30 nM), ML2 (IC₅₀ of 16 nM), EOL1 (IC₅₀ of 20 nM), and murine MLL-AF9 cells (IC₅₀ of 15 nM)) and ALL (KOPN8 (IC₅₀ of 15 nM), HB11;19 (IC₅₀ of 36 nM), MV4;11 (IC₅₀ of 17 nM), SEMK2 (IC50 of 27 nM), and RS4;11 (IC₅₀ of 25 nM)) cell lines.
At early timepoints MLL-r B cell ALL (B-ALL) cell lines, but not MLL-r AML cell lines, underwent apoptosis in response to VTP50469 in a dose-dependent manner. MLL-r AML cell lines underwent dose-dependent differentiation starting at 4-6 days of exposure to VTP50469.
VTP50469 displaces Menin from protein complexes and inhibits chromatin occupancy of MLL at select genes. Loss of MLL binding led to changes in gene expression, differentiation, and apoptosis.

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

体内研究

VTP50469 (15-60 mg/kg; oral administration; twice a day; for 28 days; NSG mice) treatment is highly efficacious across all dosage levels and all treatment groups have a significant survival advantage. Mice dosed at 30 and 60 mg/kg VTP50469 extends survival advantage.

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

Animal Model:	Unconditioned immunodeficient (NSG) mice with MV4;11 cells
Dosage:	15 mg/kg, 30 mg/kg, and 60 mg/kg
Administration:	Oral administration; twice a day; for 28 days
Result:	Was highly efficacious across all dosage levels and all treatment groups had a significant survival advantage over the control group.

体内研究

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

Animal Model:	Unconditioned immunodeficient (NSG) mice with MV4;11 cells
Dosage:	15 mg/kg, 30 mg/kg, and 60 mg/kg
Administration:	Oral administration; twice a day; for 28 days
Result:	Was highly efficacious across all dosage levels and all treatment groups had a significant survival advantage over the control group.

性状

Solid

溶解性数据

In Vitro:

DMSO : 125 mg/mL (198.15 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5852 mL	7.9262 mL	15.8524 mL
5 mM	0.3170 mL	1.5852 mL	3.1705 mL
10 mM	0.1585 mL	0.7926 mL	1.5852 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： 5% DMSO 40% PEG300 5% Tween-80 50% saline
Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution
2.

请依序添加每种溶剂： 5% DMSO 95% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (3.96 mM); Clear solution
3.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.30 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
4.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.30 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
5.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (3.30 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.30 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。