[CAS NO. 1661839-45-7] CCT251545

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PRODUCTS SPECIFICATIONS [1661839-45-7]

Catalog

SLK-S7981

Brand

Selleck

CAS

1661839-45-7

DESCRIPTION [1661839-45-7]

Overview

MDL	MFCD29472582
Molecular Weight	421.92
Molecular Formula	C23H24ClN5O
SMILES	O=C1NCCC12CCN(C3=C(Cl)C=NC=C3C4=CC=C(C5=CN(C)N=C5)C=C4)CC2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.3701 mL	11.8506 mL	23.7012 mL
5 mM	0.4740 mL	2.3701 mL	4.7402 mL
10 mM	0.2370 mL	1.1851 mL	2.3701 mL
50 mM	0.0474 mL	0.2370 mL	0.4740 mL

Description

CCT251545 is a potent, orally bioavailable inhibitor of signaling with IC50 of 5 nM in 7dF3 cells. CCT251545 also act as a selective chemical probe for exploring the role of and in human disease.

Targets

CDK8 ^[2]	CDK19 ^[2]	Wnt ^[1] (in 7dF3 cells)
		5 nM

In vitro

The suppression of the WNT pathway activity by CCT251545 is not unique to a specific cell line, is independent of exogenous WNT pathway stimulation, does not result from destabilization of TCF1 or TCF4, and is not due to interference with the luciferase-based reporter readout. CCT251545 also demonstrates a lack of transporter-mediated efflux and a lack of activity across broad in vitro panels of enzyme, receptor, and ion channel targets.

References

[1] Aurélie Mallinger, et al. J Med Chem. 2015 Feb 26;58(4):1717-35.
[2] Trevor Dale, et al. Nat Chem Biol. 2015 Dec;11(12):973-980.