Milademetan(Synonyms: DS-3032) | 赛默飞Alfa aesar官网

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

Milademetan (Synonyms: DS-3032) 纯度: 98.16%

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。

Milademetan Chemical Structure

CAS No. : 1398568-47-2

规格	价格	是否有货
10 mM * 1 mL in DMSO	￥11158	In-stock
1 mg	￥2800	In-stock
5 mg	￥8200	In-stock
10 mg	￥14000	询价
50 mg		询价
100 mg		询价

* Please select Quantity before adding items.

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^[1]^[2].

IC₅₀ & Target

MDM2^[1].

体外研究
(In Vitro)

Milademetan (DS-3032) can stabilize TP53 and selectively induce CDKNA1, BAX and MDM2 expression in neuroblastoma cells with wild-type TP53^[3].
Milademetan (DS-3032b) treatment enhances TP53 target gene expression and induces G1 cell cycle arrest, senescence and apoptosis^[3].
Milademetan (DS-3032b, 0-2000 nM) treatment selectively inhibits viability, proliferation and migration of neuroblastoma cells with wildtype TP53 independently of MYCN status^[4].

上海金畔生物科技有限公司 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].

上海金畔生物科技有限公司 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.

Clinical Trial

分子量

618.53

Formula

C₃₀H₃₄Cl₂FN₅O₄

CAS 号

1398568-47-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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。

*以上所有助溶剂都可在上海金畔生物科技有限公司网站选购。

参考文献

[1]. ARYL SULFONOHYDRAZIDES. WO 2017069289 A1.

[2]. M.M. Gounder, et al. Milademetan, an oral MDM2 inhibitor, in well-differentiated/dedifferentiated liposarcoma: results from a phase 1 study in patients with solid tumors or lymphomas. European Journal of Cancer 138S2 (2020) S1–S62.

[3]. Li, Yangbing, et al. Development of novel PROTAC Small-Molecule Degraders of MDM2 Protein and Peptidomimetic Inhibitors Targeting WDR5-MLL1 Protein-Protein Interaction.

[4]. Viktor Arnhold, et al. Reactivating TP53 signaling by the novel MDM2 inhibitor DS-3032b as a therapeutic option for high-risk neuroblastoma. ncotarget. 2018 Jan 5; 9(2): 2304–2319.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务