PROTAC CDK9 degrader-2

PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC.

Product information

CAS Number: 2435721-30-3

Molecular Weight: 748.74

Formula: C39H36N6O10

Chemical Name: 8-(4-{[(5, 7-dihydroxy-4-oxo-2-phenyl-4H-chromen-8-yl)oxy]methyl}-1H-1, 2, 3-triazol-1-yl)-N-[2-(2, 6-dioxopiperidin-3-yl)-1, 3-dioxo-2, 3-dihydro-1H-isoindol-4-yl]octanamide

Smiles: OC1C=C(O)C2=C(OC(=CC2=O)C2C=CC=CC=2)C=1OCC1=CN(CCCCCCCC(=O)NC2=CC=CC3=C2C(=O)N(C2CCC(=O)NC2=O)C3=O)N=N1

InChiKey: MRRHEHIWXXJQQL-UHFFFAOYSA-N

InChi: InChI=1S/C39H36N6O10/c46-27-18-29(48)35(36-34(27)28(47)19-30(55-36)22-10-5-4-6-11-22)54-21-23-20-44(43-42-23)17-8-3-1-2-7-14-31(49)40-25-13-9-12-24-33(25)39(53)45(38(24)52)26-15-16-32(50)41-37(26)51/h4-6,9-13,18-20,26,46,48H,1-3,7-8,14-17,21H2,(H,40,49)(H,41,50,51)

Technical Data

Appearance: Solid Power

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

Solubility: Soluble in DMSO

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

References:

1. Bian J , et al. Discovery of Wogonin-based PROTACs against CDK9 and capable of achieving antitumor activity. Bioorg Chem. 2018 Dec;81:373-381.

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