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Product details

名称

Milademetan

分子类型

小分子

别名

米拉德梅坦

英文别名

BDBM50467678 | L-erythro-Hexonamide, 2,6-anhydro-5-[[[(3'R,4'S,5'R)-6''-chloro-4'-(2-chloro-3-fluoro-4-pyridinyl)-1'',2''-dihydro-4,4-dimethyl-2''-oxodispiro[cyclohexane-1,2'-pyrrolidine-3',3''-[3H]indol]-5'-yl]carbonyl]amino]-3,4,5-trideoxy- | YFC56847 |

英文名称

Milademetan

货号

M650152-5mg

包装规格

5mg

浓度

≥98%

储存温度

-20°C储存

运输条件

超低温冰袋运输

产品介绍

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 In Vitro 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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). 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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. Form:Solid IC50& Target:MDM2

生化机理

Milademetan (DS-3032) 是一种特异性口服活性 MDM2 抑制剂，用于急性髓性白血病（AML）或实体瘤的研究。Milademetan (DS-3032) 可诱导 G1 细胞周期停滞、衰老和凋亡。

CAS号

1398568-47-2

分子式

C30H34Cl2FN5O4

分子量

618.53 g/mol

PubChem编号

73297272

Isomeric SMILES

CC1(CCC2(CC1)[C@@]3([C@H]([C@@H](N2)C(=O)N[C@@H]4CC[C@H](OC4)C(=O)N)C5=C(C(=NC=C5)Cl)F)C6=C(C=C(C=C6)Cl)NC3=O)C

INCHI

1S/C30H34Cl2FN5O4/c1-28(2)8-10-29(11-9-28)30(18-5-3-15(31)13-19(18)37-27(30)41)21(17-7-12-35-24(32)22(17)33)23(38-29)26(40)36-16-4-6-20(25(34)39)42-14-16/h3,5,7,12-13,16,20-21,23,38H,4,6,8-11,14H2,1-2H3,(H2,34,39)(H,36,40)(H,37,41)/t16-,20+,21+,23-,30-/m1/s1

InChi Key

RYAYYVTWKAOAJF-QISPRATLSA-N

Smiles

CC1(CCC2(CC1)C3(C(C(N2)C(=O)NC4CCC(OC4)C(=O)N)C5=C(C(=NC=C5)Cl)F)C6=C(C=C(C=C6)Cl)NC3=O)C

PubChem CID

73297272

关联CAS

1398568-47-2

MeSH Entry Terms

2,6-anhydro-5-((((3'R,4'S,5'R)-6''-chloro-4'-(2-chloro-3-fluoro-4-pyridinyl)-1'',2''-dihydro-4,4-dimethyl-2''-oxodispiro(cyclohexane-1,2'-pyrrolidine-3',3''-(3H)indol)-5'-yl)carbonyl)amino)-3,4,5-trideoxy-L-erythro-hexonamide;DS-3032;milademetan;RAIN-32

溶解性

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

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

617.197 Da

单同位素质量Monoisotopic Mass

617.197 Da

拓扑极表面积Topological Polar Surface Area

135.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

1090

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

3.4

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

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