Milademetan tosylate hydrate (Synonyms:DS-3032b; DS-3032 tosylate hydrate)
目录号 : KM9043 CAS No. : 2095625-97-9 纯度 : 98%

Milademetan (DS-3032) tosylate hydrate 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) tosylate hydrate 可诱导 G1 细胞周期阻滞、衰老和凋亡。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate 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.

Cell Viability Assay

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

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

Animal Model: SH-SY5Y xenograft tumors in nude mice.
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.
分子式
C37H44Cl2FN5O8S
分子量
808.74
CAS号
2095625-97-9
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 200 mg/mL (247.30 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.2365 mL 6.1825 mL 12.3649 mL
5 mM 0.2473 mL 1.2365 mL 2.4730 mL
10 mM 0.1236 mL 0.6182 mL 1.2365 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 (protect from light)。-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: 5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic

    此方案可获得 5 mg/mL (6.18 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 50.0 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。

  • 2.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 5 mg/mL (6.18 mM); Suspended solution; Need ultrasonic

    此方案可获得 5 mg/mL (6.18 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 50.0 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。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (6.18 mM); Clear solution

    此方案可获得 ≥ 5 mg/mL (6.18 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 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

临床试验
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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