Description
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.
Product information
CAS Number: 2408641-24-5
Molecular Weight: 819.87
Formula: C40H45N13O7
Chemical Name: 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)pyrazolidine-3-carboxamide
Smiles: O=C1C2C(=CC=CC=2NCCNC(=O)CCC(=O)N2CCN(CC3C=CC(=CC=3)NC(=O)C3NNCC3NC3N=CN=C4NC=CC=34)CC2)C(=O)N1C1CCC(=O)NC1=O
InChiKey: LSAODURCGYKUTN-UHFFFAOYSA-N
InChi: InChI=1S/C40H45N13O7/c54-30(42-15-14-41-27-3-1-2-25-33(27)40(60)53(39(25)59)29-8-9-31(55)49-37(29)57)10-11-32(56)52-18-16-51(17-19-52)21-23-4-6-24(7-5-23)47-38(58)34-28(20-46-50-34)48-36-26-12-13-43-35(26)44-22-45-36/h1-7,12-13,22,28-29,34,41,46,50H,8-11,14-21H2,(H,42,54)(H,47,58)(H,49,55,57)(H2,43,44,45,48)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 130 mg/mL (159.34 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
PROTAC CDK2/9 Degrader-1 (0.25-3 μM; 48 hours) induces cell cycle blockage at the G2/M phase. PROTAC CDK2/9 Degrader-1 (500 nM; 2-24 hours) down-regulates the Mcl-1 protein level in PC-3 cells. 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. PROTAC CDK2/9 Degrader-1 inhibits both CDK2 and CDK9, with IC50 as 7.42 nM and 14.50 nM, respectively.
Products are for research use only. Not for human use.
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