CCT251455


Catalog No. Size PriceQuantity
M13510-2 2mg solid $215
M13510-10 10mg solid $765

Description

CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 (MPS1) inhibitor with an IC50 of 3 nM.

Product information

CAS Number: 1400284-80-1

Molecular Weight: 503.98

Formula: C26H26ClN7O2

Chemical Name: tert-butyl 6-{[2-chloro-4-(1-methyl-1H-imidazol-5-yl)phenyl]amino}-2-(1-methyl-1H-pyrazol-4-yl)-1H-pyrrolo[3,2-c]pyridine-1-carboxylate

Smiles: CC(C)(C)OC(=O)N1C(=CC2C=NC(=CC1=2)NC1=CC=C(C=C1Cl)C1=CN=CN1C)C1C=NN(C)C=1

InChiKey: BXKNUXDLZJPPBO-UHFFFAOYSA-N

InChi: InChI=1S/C26H26ClN7O2/c1-26(2,3)36-25(35)34-21(18-12-30-33(5)14-18)9-17-11-29-24(10-22(17)34)31-20-7-6-16(8-19(20)27)23-13-28-15-32(23)4/h6-15H,1-5H3,(H,29,31)

Technical Data

Appearance: Solid Power

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

Solubility: 10 mM in DMSO

Shipping Condition: Shipped under ambien...

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:

CCT251455 is a highly potent inhibitor of MPS1 that demonstrates high selectivity versus kinases tested in a broad kinome profiling panel. CCT251455 inhibits P-MPS1 with an IC50 of 0.04 μM in cell-based assay and has a GI50 of 0.16 μM.

In Vivo:

CCT251455 demonstrates a good oral pharmacokinetic profile in mouse and rat as well as inhibition of MPS1 activity in vivo following oral administration.

References:

  1. Naud S, et al. Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). J Med Chem. 2013 Dec 27;56(24):10045-65.

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

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