[CAS NO. 1542705-92-9]  CB-5083

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PRODUCTS SPECIFICATIONS [1542705-92-9]

Store
Catalog
SLK-S8101
Brand
Selleck
CAS
1542705-92-9

DESCRIPTION [1542705-92-9]

Overview

MDLMFCD28963914
Molecular Weight413.47
Molecular FormulaC24H23N5O2
SMILESO=C(C1=CC=CC2=C1C=C(C)N2C3=NC(NCC4=CC=CC=C4)=C(COCC5)C5=N3)N

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

1 mg5 mg10 mg
1 mM2.4186 mL12.0928 mL24.1856 mL
5 mM0.4837 mL2.4186 mL4.8371 mL
10 mM0.2419 mL1.2093 mL2.4186 mL
50 mM0.0484 mL0.2419 mL0.4837 mL

Description

CB-5083 is a potent, selective, and orally bioavailable inhibitor with of 11 nM. Phase 1.

Targets

p97 AAA ATPase [1]
(Cell-free assay)
11 nM

In vitro

In A549 cells, CB-5083 causes significant K48 poly-ubiquitinated protein and CHOP accumulation as well as p62 reduction, and kills tumor cells with IC50 of 680 nM.

In vivo

In mice bearing human HCT 116 colon tumor xenografts, CB-5083 (75 mg/kg, p.o.) significantly inhibits tumor growth. In mice bearing established human AMO-1 multiple myeloma and A549 lung carcinoma tumor xenografts, CB-5083 (100 mg/kg, p.o.) also results in significant tumor growth inhibition.