c-MET PROTAC D15

Chemical Structure : c-MET PROTAC D15

CAS No.: 2959535-15-8

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货号: PC-27354Not For Human Use, Lab Use Only.

c-MET PROTAC D15 is a potent, selective and orally active c-MET PROTAC degrader with DC50 of 0.44 nM and 0.35 nM in EBC-1 and Hs746T cells respectively (Dmax >99%).

规格	价格	库存
1 mg	￥3280	In stock
2 mg	￥5280	In stock
5 mg		Get quote
10 mg		Get quote
25 mg		Get quote

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生物&药学活性

c-MET PROTAC D15 is a potent, selective and orally active c-MET PROTAC degrader with DC50 of 0.44 nM and 0.35 nM in EBC-1 and Hs746T cells respectively (Dmax >99%).
D15 exhibits antiproliferative effect for c-Met sensitive EBC-1 and Hs746T cells with IC50 of 2.11 nM and 3.50 nM respectively.
D15 degraders c-MET through the ubiquitin proteasome pathway and the formation of ternary complex.
D15 (10 nM) significantly inhibits cell migration and invasion in EBC-1 and Hs746T cells.
D15 (10-100 nM) induces apoptosis and G1 cell cycle arrest in BC-1 and Hs746T cells.
D15 (10 mg/kg, i.p.) significantly inhibited EBC-1 tumor growth in vivo.
D15 (p.o., 40 mg/kg) significantly repressed Hs746T tumor growth in vivo.

物理化学性质&存储条件

分子量	860.93
分子式	C47H44N10O7
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	Benzonitrile, 3-[1-[[3-[5-[[1-[2-[4-[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-5-yl]-1-piperazinyl]-2-oxoethyl]-4-piperidinyl]methoxy]-2-pyrimidinyl]phenyl]methyl]-1,6-dihydro-6-oxo-3-pyridazinyl]-

参考文献

1. Pengyun Li, et al. Acta Pharm Sin B. 2023 Jun;13(6):2715-2735.

2. Patent CN116496253 A 2023-07-28.

c-MET PROTAC D15

生物&药学活性

物理化学性质&存储条件

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