CB-5083, p97 AAA ATPase Inhibitor


Catalog No. size PriceQuantity
M60306-2S 2 mg solid $129
M60306-10S 10 mg solid $516

Description

CB-5083 is a novel first in class, potent orally bio-available p97 inhibitor that disrupts cellular protein homeostasis and demonstrates anti-tumor activity in solid and hematological models . CB-5083 causes rapid and sustained accumulation of poly-ubiquitin in tumor xenografts after a single administration. CB-5083 showed activity to inhibit tumor growth in multiple rodent models of human cancer. Furthermore, CB-5083 appears to exhibit greater potency over current proteasome inhibitors that further validate targeting p97 and protein homeostasis in the treatment of cancer.

Product information

CAS Number: 1542705-92-9

Molecular Weight: 413.47

Formula: C24H23N5O2

Chemical Name: 1-(4-(benzylamino)-7,8-dihydro-5H-pyrano[4,3-d]pyrimidin-2-yl)-2-methyl-1H-indole-4-carboxamide

Smiles: CC1=CC2C(=CC=CC=2C(N)=O)N1C1=NC2CCOCC=2C(NCC2C=CC=CC=2)=N1

InChiKey: RDALZZCKQFLGJP-UHFFFAOYSA-N

InChi: InChI=1S/C24H23N5O2/c1-15-12-18-17(22(25)30)8-5-9-21(18)29(15)24-27-20-10-11-31-14-19(20)23(28-24)26-13-16-6-3-2-4-7-16/h2-9,12H,10-11,13-14H2,1H3,(H2,25,30)(H,26,27,28)

Technical Data

Appearance: Solid Power.

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

Solubility: DMSO up to 100 mM

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: ≥360 days 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:

CB-5083 was used at 1-2.5 µM final concentration in various assays.

In Vivo:

CB-5083 was dosed to mice orally at 25-100 mg/Kg once or twice per day.

References:

  1. Zhou HJ, et al. Discovery of a First-in-Class, Potent, Selective, and Orally Bioavailable Inhibitor of the p97 AAA ATPase (CB-5083). (2015) J Med Chem. 58(24):9480-97.

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

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