CP-10, PROTAC for CDK6

CP-10 is a PROTAC with highly selective, specific, and remarkable CDK6 degradation (DC50=2.1 nM). It inhibits proliferation of several haematopoietic cancer cells with impressive potency including multiple myeloma, and can still degrades mutated and overexpressed CDK6

Product information

CAS Number: 2366268-80-4

Molecular Weight: 871.94

Formula: C44H49N13O7

Chemical Name: 4-[(2-{2-[4-({4-[6-({6-acetyl-8-cyclopentyl-5-methyl-7-oxo-7H,8H-pyrido[2,3-d]pyrimidin-2-yl}amino)pyridin-3-yl]piperazin-1-yl}methyl)-1H-1,2,3-triazol-1-yl]ethoxy}ethyl)amino]-2-(2,6-dioxopiperidin-3-yl)-2,3-dihydro-1H-isoindole-1,3-dione

Smiles: CC(=O)C1C(=O)N(C2CCCC2)C2=NC(NC3=CC=C(C=N3)N3CCN(CC4=CN(CCOCCNC5=CC=CC6=C5C(=O)N(C5CCC(=O)NC5=O)C6=O)N=N4)CC3)=NC=C2C=1C

InChiKey: PACRWHUPEPCFHX-UHFFFAOYSA-N

InChi: InChI=1S/C44H49N13O7/c1-26-32-23-47-44(50-39(32)56(29-6-3-4-7-29)42(62)37(26)27(2)58)48-35-12-10-30(22-46-35)54-17-15-53(16-18-54)24-28-25-55(52-51-28)19-21-64-20-14-45-33-9-5-8-31-38(33)43(63)57(41(31)61)34-11-13-36(59)49-40(34)60/h5,8-10,12,22-23,25,29,34,45H,3-4,6-7,11,13-21,24H2,1-2H3,(H,49,59,60)(H,46,47,48,50)

Technical Data

Appearance: Solid Power

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

Solubility: DMSO : 200 mg/mL (229.37 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:

CP-10 induces nearly 72% degradation of CDK6 at 10 nM and 89% at 100 nM in human glioblastoma U251 cells. The degradation of CDK4 induced by CP-10 is far weaker than that of CDK6 (DC50: 50-80 fold). CP-10 displays a cell inhibition potential in multiple myeloma cell MM.1S (IC50≈10 nM) and mantle cell lymphoma cells (in Mino, IC50≈8 nM).

References:

1. Su S, et al. Potent and Preferential Degradation of CDK6 via Proteolysis Targeting Chimera Degraders. J Med Chem. 2019 Aug 2.

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