AVN-944 VX-944|cas:297730-17-7|西域试剂

AVN-944 VX-944,99.77%

产品编号：Bellancom-13560| CAS NO：297730-17-7| 分子式：C₂₅H₂₇N₅O₅| 分子量：477.51

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-13560	￥1133.00	杭州北京（现货）
Bellancom-13560	￥1700.00	杭州北京（现货）
Bellancom-13560	￥2450.00	杭州北京（现货）
Bellancom-13560	￥7500.00	杭州北京（现货）

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AVN-944 VX-944

产品介绍

AVN-944 (VX-944) 是一种口服有效、选择性、非竞争性和特异性的 IMPDH (肌苷一磷酸脱氢酶)抑制剂。AVN-944 是从头合成鸟嘌呤核苷酸的必要限速酶。AVN-944 也是一种沙粒病毒 RNA 合成 (arenavirus RNA synthesis) 抑制剂，可阻断沙粒病毒感染。AVN-944 具有广泛的抗癌活性，可用于多发性骨髓瘤 (MM) 和急性髓系白血病 (AML) 的研究。

生物活性

AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research.

体外研究

AVN-944 (0-1 μM, 48 h) inhibits growth of human multiple myeloma (MM) cell lines in a dose-dependent manner.
AVN-944 (800 nM, 0-72 h) induces apoptosis in MM cell lines via a caspase-independent, Bax/AIF/Endo G pathway.
AVN-944 (0-200 nM) enhances the cytotoxicity of Doxorubicin (HY-15142A) and Melphalan (HY-17575).
AVN-944 inhibits the proliferation of the human MV-4-11 and murine Ba/F3-Flt3-ITD-dependent cell lines with IC₅₀ values of 26 and 30 nM, respectively.
AVN-944 (0-32 μM, 48 h) shows good activity against arenavirus infection at low doses (7.5 μM) with less cytotoxicity.
AVN-944 (0-6.4 μM, 48 h) does not reduce the viability of peripheral blood mononuclear cells (PBMNCs).

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

Cell Proliferation Assay

Cell Line:	RPMI8226, MM.1S, and U266 cells
Concentration:	0, 100, 200, 300, 400, 600, 1000 nM
Incubation Time:	48 h
Result:	Significantly inhibited the growth of RPMI8226, MM.1S, and U266 cells in a dose-dependent fashion, with 50% inhibition (IC₅₀) values at 48 h of 450, 450, and 600 nM, respectively. Inhibited growth of drug-resistant cell lines, including Doxorubicin (Dox)-resistant RPMI8226-Dox40, Melphalan (Mel) resistant RPMI8226-LR5, and Dex (Dexamethasone) resistant MM.1R cells, with IC₅₀ values similar to the parental drug-sensitive cell lines.

Apoptosis Analysis

Cell Line:	MM.1S and RPMI8226 cells
Concentration:	800 nM
Incubation Time:	48 and 72 h
Result:	Induced apoptosis in MM cell lines.

Western Blot Analysis

Cell Line:	MM.1S and RPMI8226 cells
Concentration:	800 nM
Incubation Time:	12, 24, 48 h
Result:	Induced modest cleavage of caspase 3, 8 and 9 in MM.1S cells and RPMI8226 cells. Markedly upregulated Bax and Bak, without significant changes in Bcl-2, Mcl-1, XIAP, and Bad. Observed translocation of mitochondrial proapoptotic proteins, apoptosis-inducing factor (AIF) and endonuclease G (Endo G) to cytosolic fractions.

Cell Cytotoxicity Assay

Cell Line:	MM.1S cells, MM.1S cells cultured with BMSCs
Concentration:	0, 50, 200 nM
Incubation Time:	24 h
Result:	Enhanced the cytotoxicity of of Doxorubicin and Melphalan in MM.1S cells. Additive effects were also observed in MM.1S cells cultured with BMSCs derived from MM patient.

体内研究
(In Vivo)

AVN-944 (0-150 mg/kg, Orally, twice daily) significantly increases the median survival time of leukemia model mice.

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

Animal Model:	Balb/c mice (leukemia model, using Ba/F3 cells transduced with an activating human Flt-3 mutation injected into mice)
Dosage:	75 or 150 mg/kg
Administration:	Orally, twice daily
Result:	Provided a significant increase in median survival time. Three of the 12 mice treated with 150 mg/kg AVN-944 were still alive on Day 35 when the study was terminated.

体内研究

AVN-944 (0-150 mg/kg, Orally, twice daily) significantly increases the median survival time of leukemia model mice.

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

Animal Model:	Balb/c mice (leukemia model, using Ba/F3 cells transduced with an activating human Flt-3 mutation injected into mice)
Dosage:	75 or 150 mg/kg
Administration:	Orally, twice daily
Result:	Provided a significant increase in median survival time. Three of the 12 mice treated with 150 mg/kg AVN-944 were still alive on Day 35 when the study was terminated.

体内研究

AVN-944 (0-150 mg/kg, Orally, twice daily) significantly increases the median survival time of leukemia model mice.

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

Animal Model:	Balb/c mice (leukemia model, using Ba/F3 cells transduced with an activating human Flt-3 mutation injected into mice)
Dosage:	75 or 150 mg/kg
Administration:	Orally, twice daily
Result:	Provided a significant increase in median survival time. Three of the 12 mice treated with 150 mg/kg AVN-944 were still alive on Day 35 when the study was terminated.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (209.42 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0942 mL	10.4710 mL	20.9420 mL
5 mM	0.4188 mL	2.0942 mL	4.1884 mL
10 mM	0.2094 mL	1.0471 mL	2.0942 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: ≥ 2.5 mg/mL (5.24 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.24 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.24 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.24 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。