PROTAC CDK2/9 Degrader-1
- Product Name
- PROTAC CDK2/9 Degrader-1
- CAS No.
- 2408641-24-5
- Chemical Name
- PROTAC CDK2/9 Degrader-1
- Synonyms
- PROTAC CDK2;PROTAC CDK2/9 Degrader-1;4-((7H-Pyrrolo[2,3-d]pyrimidin-4-yl)amino)-N-(4-((4-(4-((2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)amino)-4-oxobutanoyl)piperazin-1-yl)methyl)phenyl)-1H-pyrazole-3-carboxamide;N-{4-[(4-{3-[(2-{[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxo-2,3-dihydro-1H-isoindol-4-yl]amino}ethyl)carbamoyl]propanoyl}piperazin-1-yl)methyl]phenyl}-4-({7H-pyrrolo[2,3-d]pyrimidin-4-yl}amino)-1H-pyrazole-3-carboxamide
- CBNumber
- CB28054502
- Molecular Formula
- C40H41N13O7
- Formula Weight
- 815.84
- MOL File
- Mol file
PROTAC CDK2/9 Degrader-1 Property
- Density
- 1.534±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 130 mg/mL (159.34 mM; Need ultrasonic)
- form
- Solid
- pka
- 10.74±0.40(Predicted)
- color
- White to yellow
PROTAC CDK2/9 Degrader-1 Chemical Properties,Usage,Production
Biological Activity
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 (DC50=62 nM) and CDK9 (DC50=33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC50=0.12 μM) by effectively blocking the cell cycle in S and G2/M phases. PROTAC CDK2/9 Degrader-1 is a PROTAC by tethering CDK inhibitor with CRBN ligand[1]. PROTAC CDK2/9 Degrader-1 (0.25-3 μM; 48 hours) induces cell cycle blockage at the G2/M phase[1].PROTAC CDK2/9 Degrader-1 (500 nM; 2-24 hours) down-regulates the Mcl-1 protein level in PC-3 cells[1].PROTAC CDK2/9 Degrader-1 effectively degrades CDK2/9 in cell lines MCF-7, HCT-116 and 22Rv1, which all have high CDK2/9 expression[1].PROTAC CDK2/9 Degrader-1 inhibits both CDK2 and CDK9, with IC50 as 7.42 nM and 14.50 nM, respectively[1].
References
[1]. Zhou F, et al. Development of selective mono or dual PROTAC degrader probe of CDK isoforms. Eur J Med Chem. 2019 Dec 6;187:111952.
PROTAC CDK2/9 Degrader-1 Preparation Products And Raw materials
Raw materials
Preparation Products
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