[CAS NO. 2408641-24-5] PROTACCDK2/9Degrader-1
PRODUCTS SPECIFICATIONS [2408641-24-5]
DESCRIPTION [2408641-24-5]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 815.84 |
| Molecular Formula | C40H41N13O7 |
| SMILES | O=C(C1=NNC=C1NC2=C3C(NC=C3)=NC=N2)NC4=CC=C(CN5CCN(C(CCC(NCCNC6=CC=CC(C(N7C(CC8)C(NC8=O)=O)=O)=C6C7=O)=O)=O)CC5)C=C4 |
Summary
PROTAC CDK2/9 Degrader-1 (Compound F3) is a potent dual degrader for CDK2 ( DC 50 =62 nM) and CDK9 ( DC 50 =33 nM). PROTAC CDK2/9 Degrader-1 suppresses prostate cancer PC-3 cell proliferation (IC 50 =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] .
IC50 & Target
|
CDK2 62 nM (DC 50 ) |
CDK9 33 nM (DC 50 ) |
Cereblon
|
In Vitro
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 IC
50
as 7.42 nM and 14.50 nM, respectively
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Cycle Analysis [1]
| Cell Line: | PC-3 cells |
| Concentration: | 500 nM |
| Incubation Time: | 2, 4, 8, 16, 24 hours |
| Result: | Down-regulated the Mcl-1 protein level in PC-3 cells. |
Western Blot Analysis [1]
| Cell Line: | PC-3 cells |
| Concentration: | 0.25, 1, 3 μM |
| Incubation Time: | 48 hours |
| Result: | Induced cell cycle blockage at the G2/M phase. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 55 mg/mL ( 67.42 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.2257 mL | 6.1287 mL | 12.2573 mL |
| 5 mM | 0.2451 mL | 1.2257 mL | 2.4515 mL |
| 10 mM | 0.1226 mL | 0.6129 mL | 1.2257 mL |
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1.