| Identification | Back Directory | [Name]
PROTAC CDK2/9 Degrader-1 | [CAS]
2408641-24-5 | [Synonyms]
PROTAC CDK2
PROTAC CDK2/9 Degrader-1 | [Molecular Formula]
C40H41N13O7 | [MDL Number]
MFCD34179485 | [MOL File]
2408641-24-5.mol | [Molecular Weight]
815.84 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
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 Cereblon ligand[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]. | [IC 50]
CDK2: 62 nM (DC50); CDK9: 33 nM (DC50); Cereblon | [storage]
Store at -20°C | [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. |
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| Company Name: |
cjbscvictory
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| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
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