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VTP50469 fumarate

产品编号 T13336L CAS 2169919-29-1

VTP50469 fumarate is a highly selective and orally active inhibitor of Menin-MLL interaction (Ki: 104 pM), and has potently anti-leukemia activity.

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VTP50469 fumarate, CAS 2169919-29-1

规格	价格/CNY		货期	数量
25 mg	￥ 8,430		待询

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VTP50469 fumarate 的其他形式现货产品:

VTP50469

其他形式的 VTP50469 fumarate:

VTP50469
现货
VTP50469 mesylate
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参考文献

产品描述	VTP50469 fumarate is a highly selective and orally active inhibitor of Menin-MLL interaction (Ki: 104 pM), and has potently anti-leukemia activity.
靶点活性	Menin-MLL:ki:104 pM
体外活性	VTP50469 more potently and rapidly inhibits cell proliferation in a concentration-dependent manner in MLL-r cell lines carrying (MOLM13 with IC50 of 13 nM), THP1 with IC50 of 37 nM, NOMO1 with 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[1]. 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[1]. VTP50469 replaces Menin in protein complexes and suppresses the chromatin occupancy of MLL on certain genes. Loss of MLL binding leads to changes in gene expression, differentiation and apoptosis[1].
体内活性	In NSG mice, VTP50469 (15-60 mg/kg; oral administration; twice a day; for 28 days) 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[1].

分子量	1609.86
分子式	C76H106F2N12O20S2
CAS No.	2169919-29-1

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Krivtsov AV, et al. A Menin-MLL Inhibitor Induces Specific Chromatin Changes and Eradicates Disease in Models of MLL-Rearranged Leukemia. Cancer Cell. 2019 Dec 9;36(6):660-673.e11. 2. Andrei V. Krivtsov, et al. Abstract 4958: VTP50469 is a novel, orally available menin-MLL1 inhibitor effective against MLL-rearranged and NPM1-mutant leukemia. Cancer Resceach. July 2018.Volume 78, Issue 13 Supplement.

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请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

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