MI-773(2'S,3R isomer,SAR-405838) - �뵺�羺�ٷ��ַ

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MI-773(2'S,3R isomer,SAR-405838)

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验、�/div>

CAS NO:	1303607-60-4
规格:	�?8%

包装与价格：

包装	价格(�?
2mg	电议
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议

产品介绍

理化性质和储存条仵�/div>

Molecular Weight (MW)	562.50
Formula	C29H34Cl2FN3O3
CAS No.	1303607-60-4
Storage	-20� for 3 years in powder form
Storage	-80� for 2 years in solvent
Solubility(In vitro)	DMSO: 100 mg/mL (177.77 mM)
	Water:<1 mg/mL (slightly soluble or insoluble)
	Ethanol: 31 mg/mL warming (55.11 mM)
Other info	InChi Key: IDKAKZRYYDCJDU-HBMMIIHUSA-N InChi Code: InChI=1S/C29H34Cl2FN3O3/c1-28(2,3)14-22-29(19-12-7-15(30)13-21(19)34-27(29)38)23(18-5-4-6-20(31)24(18)32)25(35-22)26(37)33-16-8-10-17(36)11-9-16/h4-7,12-13,16-17,22-23,25,35-36H,8-11,14H2,1-3H3,(H,33,37)(H,34,38)/t16-,17-,22-,23-,25+,29+/m0/s1 SMILES Code: O=C([C@H](N[C@H]1CC(C)(C)C)[C@H](C2=CC=CC(Cl)=C2F)[C@@]31C(NC4=C3C=CC(Cl)=C4)=O)N[C@H]5CC[C@H](O)CC5
Chemical Name/Synonyms	(2'S,3R,4'S,5'R)-6-chloro-4'-(3-chloro-2-fluorophenyl)-N-((1r,4R)-4-hydroxycyclohexyl)-2'-neopentyl-2-oxospiro[indoline-3,3'-pyrrolidine]-5'-carboxamide; SAR-405838; SAR 405838; SAR405838; MI-773; MI773; MI 773

实验参考方泔�/div>

In Vitro	MI-773 potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092 μM), RS4;11 (IC50, 0.089 μM), LNCaP (IC50, 0.27 μM), and HCT-116 (IC50, 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50,>10 μM), PC-3 (IC50,>10 μM), SW620 (IC50,>10 μM), and HCT-116 (p53-/-) (IC50,>20 μM) cells
In Vivo	In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, MI-773 (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg).
Animal model	SCID mice with SJSA-1 osteosarcoma (females), acute lymphoblastic leukemia RS4;11 (females), LNCaP prostate cancer (males), or HCT-116 colon cancer (females) xenograft model
Formulation & Dosages	10% PEG400: 3% Cremophor: 87% PBS, or 2% TPGS: 98% PEG200; 200 mg/kg; Oral
References	[1] Wang S, et al. Cancer Res. 2014, 74(20), 5855-5865.

生物活�?/div>

Microsoft Word - NIHMS621402-manuscript-1SAR405838 potently activates p53 in the SJSA-1 and HCT-116 cancer cell lines and strongly induces PUMA up-regulation and cleavage of caspase-3 and PARP in the SJSA-1 cell line but not in the HCT-116 cell line. Wang S, et al. Cancer Res. 2014, 74(20), 5855-5865.