PROTAC CDK2/9 Degrader-1
- CAS NO.:2408641-24-5
- Empirical Formula: C40H41N13O7
- Molecular Weight: 815.84
- MDL number: MFCD34179485
- Update Date: 2024-07-02 08:55:04
What is PROTAC CDK2/9 Degrader-1?
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.
Properties of PROTAC CDK2/9 Degrader-1
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 |
Safety information for PROTAC CDK2/9 Degrader-1
Computed Descriptors for PROTAC CDK2/9 Degrader-1
New Products
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