CRA-026440

Product NameCRA-026440
CAS847460-34-8
MFC23H24N4O4
MW420.46
EINECS
MOL File847460-34-8.mol

Chemical Properties

Density	1.35±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	Soluble in DMSO
pka	8.71±0.10(Predicted)

Usage And Synthesis

Uses

CRA-026440 is a potent, broad-spectrum HDAC inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4, 14, 11, 15, 7, and 20 nM respectively. CRA-026440 shows antitumor and antiangiogenic activities[1]. CRA-026440 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

in vivo

CRA-026440 (100 mg/kg; i.v.; daily; for three consecutive days) results in a statistically significant reduction in tumor growth in mice harboring HCT116 or U937 human tumor xenografts^[1].

Animal Model:	HCT-116 tumor-bearing nude mice^[1]
Dosage:	100 mg/kg
Administration:	i.v.; daily; for three consecutive days
Result:	Resulted in a statistically significant reduction in tumor growth.

IC 50

HDAC1: 4 nM (Ki); HDAC8: 7 nM (Ki); HDAC3: 11 nM (Ki); HDAC2: 14 nM (Ki); HDAC6: 15 nM (Ki); HDAC10: 20 nM (Ki)

References

[1] Cao ZA, et al. CRA-026440: a potent, broad-spectrum, hydroxamic histone deacetylase inhibitor with antiproliferative and antiangiogenic activity in vitro and in vivo. Mol Cancer Ther. 2006 Jul;5(7):1693-701. DOI:10.1158/1535-7163.MCT-06-0042