CP5V is a PROTAC, which specifically degrades Cdc20 by linking Cdc20 to the VHL/VBC complex for ubiquitination followed by proteasomal degradation. CP5V induces mitotic inhibition and suppresses cancer cell proliferation.

Product information

CAS Number: 2509359-75-3

Molecular Weight: 1075.49

Formula: C46H66Cl3N9O12S

Chemical Name: 3-(1-{[(2S)-1-[(2S,4R)-4-hydroxy-2-({[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl}carbamoyl)pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl}-3,6,9,12,15-pentaoxaoctadecan-18-amido)propyl N-{2,2,2-trichloro-1-[(pyrimidin-2-yl)amino]ethyl}carbamate

Smiles: CC(C)(C)[C@H](NC(=O)CCOCCOCCOCCOCCOCCC(=O)NCCCOC(=O)NC(NC1N=CC=CN=1)C(Cl)(Cl)Cl)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCC1C=CC(=CC=1)C1SC=NC=1C

InChiKey: BQQILUVLGKHSNJ-NWRQRLFSSA-N

InChi: InChI=1S/C46H66Cl3N9O12S/c1-31-38(71-30-54-31)33-9-7-32(8-10-33)28-53-40(62)35-27-34(59)29-58(35)41(63)39(45(2,3)4)55-37(61)12-18-66-20-22-68-24-26-69-25-23-67-21-19-65-17-11-36(60)50-15-6-16-70-44(64)57-42(46(47,48)49)56-43-51-13-5-14-52-43/h5,7-10,13-14,30,34-35,39,42,59H,6,11-12,15-29H2,1-4H3,(H,50,60)(H,53,62)(H,55,61)(H,57,64)(H,51,52,56)/t34-,35+,39-,42?/m1/s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 150 mg/mL (139.47 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:

CP5V comprises a Cdc20 ligand and VHL binding moiety bridged by a PEG5 linker that induces Cdc20 degradation. CP5V induces degradation of Cdc20 leading to significant inhibition of breast cancer cell proliferation and resensitization of Taxol-resistant cell lines. CP5V profoundly degrades Cdc20 in both MCF7 and MDA-MB-231 cells with DC50 being approximately 1.6 μM.

Products are for research use only. Not for human use.