CID-2011756

CID-2011756 is a cell-active ATP competitive and specific PKD1 inhibitor that inhibits phorbol ester-induced endogenous PKD1 activation in LNCaP prostate cancer cells. IC50 Value: 10±0.7 uM (cellular inhibition of phospho-Ser916-PKD1 activity) [1] Target: PKD CID 2011756, has pan-PKD inhibitory effects (PKD2 IC50 = 0.6±0.1 uM; PKD3 IC50 = 0.7±0.2 uM) with similar, albeit not identical, potencies which may be expected for an ATP competitive inhibitor. CID 2011756 was the most potent of the inhibitors with a cellular EC50 of 10±0.7 uM (n = 3), an EC50 value comparable to that of our previously described benzoxoloazepinolone.

Product information

CAS Number: 638156-11-3

Molecular Weight: 396.87

Formula: C22H21ClN2O3

Chemical Name: 5-(3-chlorophenyl)-N-(4-(morpholinomethyl)phenyl)furan-2-carboxamide

Smiles: O=C(NC1=CC=C(CN2CCOCC2)C=C1)C1=CC=C(O1)C1=CC(Cl)=CC=C1

InChiKey: XQJWTJLJEYIUDZ-UHFFFAOYSA-N

InChi: InChI=1S/C22H21ClN2O3/c23-18-3-1-2-17(14-18)20-8-9-21(28-20)22(26)24-19-6-4-16(5-7-19)15-25-10-12-27-13-11-25/h1-9,14H,10-13,15H2,(H,24,26)

Technical Data

Appearance: Solid Power

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

Solubility: 10 mM 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. Sharlow ER, et al. Discovery of diverse small molecule chemotypes with cell-based PKD1 inhibitory activity. PLoS One. 2011;6(10):e25134.

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