D16-M1P2

Chemical Structure : D16-M1P2

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货号: PC-25851Not For Human Use, Lab Use Only.

D16-M1P2 is a potent, highly specific, bifunctional PKMYT1-targeting PROTAC degrader with DC50 of 0.7 nM and Dmax of 90% in HCC1569 cells.

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生物&药学活性

D16-M1P2 is a potent, highly specific, bifunctional PKMYT1-targeting PROTAC degrader with DC50 of 0.7 nM and Dmax of 90% in HCC1569 cells.
D16-M1P2 inhibits pCDK1 (T14) in HCC1569 cells with IC50 of 9.0 nM.
D16-M1P2 (100 M) caused rapid PKMYT1 degradation, reducing PKMYT1 levels by over 80% within 4 hours and reaching maximal degradation at 24 hours.
D16-M1P2 time-dependently inhibited pCDK1 (T14), achieving over 50% inhibition after 4 hours of treatment at 100 nM.
D16-M1P2 demonstrates dual degradation and inhibition for PKMYT1, shows PKMYT1 enzymatic inhibition (IC50=7.6nM) and intracellular target engagement (EC50=12.0 nM).
D16-M1P2 exhibits high specificity for PKMYT1 with over 50-fold selectivity over only 3 kinases (BRAF, RAF1, and SRC) in 403 kinases panel.
D16-M1P2 inhibits the growth of tumors with CCNE1 amplification or deleterious alterations in FBXW7/PPP2R1A (IC50=177 nM), 12-fold greater selectivity over wild-type cells.
D16-M1P2 exhibited dose-dependent tumor growth inhibition, achieving 35.1% and 66.4% inhibition at 40 mg/kg and 120 mg/kg dosed twice daily for 21 days in NOD/SCID mice with subcutaneous CCNE1-amplified HCC1569 tumors, induced dose-dependent PKMYT1 degradation and corresponding pCDK1 (T14) inhibition with favorable plasma exposure.

物理化学性质&存储条件

分子量	784.90
分子式	C43H45FN10O4
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	(5R)-2-(2-(3-(4-(4-(((S)-2,6-dioxopiperidin-3-yl)amino)-2-fluorophenyl)piperazin-1-yl)-1-oxa-8-azaspiro[4.5]decan-8-yl)pyrimidin-5-yl)-5-(3-hydroxy-2,6-dimethylphenyl)-1H-pyrrolo[2,3-b]pyridine-4-carbonitrile

参考文献

1. Yazhou Wang, et al. Nat Commun. 2025 Nov 28;16(1):10759.

D16-M1P2

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D16-M1P2

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