Milademetan DS-3032|cas:1398568-47-2|西域试剂

Milademetan DS-3032,98.77%

产品编号：Bellancom-101266| CAS NO：1398568-47-2| 分子式：C₃₀H₃₄Cl₂FN₅O₄| 分子量：618.53

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货号	价格	库存与货期
Bellancom-101266	￥2800.00	杭州北京（现货）
Bellancom-101266	￥8200.00	杭州北京（现货）
Bellancom-101266	￥14000.00	杭州北京（现货）

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Milademetan DS-3032

产品介绍

Milademetan (DS-3032) 是特异性的、具有口服活性的 MDM2 抑制剂，用于急性髓系白血病和实体肿瘤的研究。Milademetan (DS-3032) 可诱导 G1 细胞周期阻滞、衰老和凋亡。

生物活性

Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.

体外研究

Milademetan (DS-3032) can stabilize TP53 and selectively induce CDKNA1, BAX and MDM2 expression in neuroblastoma cells with wild-type TP53.
Milademetan (DS-3032b) treatment enhances TP53 target gene expression and induces G1 cell cycle arrest, senescence and apoptosis.
Milademetan (DS-3032b, 0-2000 nM) treatment selectively inhibits viability, proliferation and migration of neuroblastoma cells with wildtype TP53 independently of MYCN status^[4].

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

Cell Viability Assay^[4]

Cell Line:	SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines.
Concentration:	0-2000 nM.
Incubation Time:	24-72 h.
Result:	Reduced viability in a dose- and time-dependent manner. Exhibited IC50 values of 21.9 nM, 17.7 nM, 52.63 nM, 25.7 nM and 44.1 nM in SK-N-SH, SH-SY5Y, IMR32, IMR5 and LAN5 cell lines, respectively (72 h).

体内研究
(In Vivo)

Milademetan (DS-3032b, 50 mg/kg, oral gavage) delays tumor growth and improves survival in mice xenografted with neuroblastoma cells with functional TP53^[4].

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

Animal Model:	SH-SY5Y xenograft tumors in nude mice^[4].
Dosage:	50 mg/kg.
Administration:	Oral gavage for 30 consecutive days with an alternating schedule of 4 days of daily treatment with oral gavages followed by 2 days without treatment (4+2).
Result:	Survival in the mouse cohort was significantly prolonged. Reduced neuroblastoma xenograft tumor growth by activating TP53 signaling.

体内研究

Milademetan (DS-3032b, 50 mg/kg, oral gavage) delays tumor growth and improves survival in mice xenografted with neuroblastoma cells with functional TP53^[4].

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

Animal Model:	SH-SY5Y xenograft tumors in nude mice^[4].
Dosage:	50 mg/kg.
Administration:	Oral gavage for 30 consecutive days with an alternating schedule of 4 days of daily treatment with oral gavages followed by 2 days without treatment (4+2).
Result:	Survival in the mouse cohort was significantly prolonged. Reduced neuroblastoma xenograft tumor growth by activating TP53 signaling.

体内研究

Milademetan (DS-3032b, 50 mg/kg, oral gavage) delays tumor growth and improves survival in mice xenografted with neuroblastoma cells with functional TP53^[4].

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

Animal Model:	SH-SY5Y xenograft tumors in nude mice^[4].
Dosage:	50 mg/kg.
Administration:	Oral gavage for 30 consecutive days with an alternating schedule of 4 days of daily treatment with oral gavages followed by 2 days without treatment (4+2).
Result:	Survival in the mouse cohort was significantly prolonged. Reduced neuroblastoma xenograft tumor growth by activating TP53 signaling.

性状

Solid

溶解性数据

In Vitro:

DMSO : 16.67 mg/mL (26.95 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.6167 mL	8.0837 mL	16.1674 mL
5 mM	0.3233 mL	1.6167 mL	3.2335 mL
10 mM	0.1617 mL	0.8084 mL	1.6167 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: ≥ 1.67 mg/mL (2.70 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (2.70 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 16.7 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: 1.67 mg/mL (2.70 mM); Suspended solution; Need ultrasonic

此方案可获得 1.67 mg/mL (2.70 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 16.7 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: ≥ 1.67 mg/mL (2.70 mM); Clear solution

此方案可获得 ≥ 1.67 mg/mL (2.70 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 16.7 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。