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抑制剂 > 免疫学/炎症 > Milademetan tosylate hydrate
产品名称:
Milademetan tosylate hydrate
型号:
CS-01Y77501
生产地址
进口、国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

5 mg 10 mg 25 mg 50 mg 100 mg

CAS

2095625-97-9

别名

N/A

化学名

N/A

分子式

C37H44Cl2FN5O8S

分子量

808.74

溶解度

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

储存条件

4°C, protect from light

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                            

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[1][2].

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].

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

[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.

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:Milademetan tosylate hydrate 

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