| Identification | Back Directory | [Name]
1H-Indole-2-carboxamide, 5-[2-(dimethylamino)ethoxy]-N-[3-[4-[(hydroxyamino)carbonyl]phenyl]-2-propyn-1-yl]-, hydrochloride (1:1) | [CAS]
847459-98-7 | [Synonyms]
HDAC/BET-IN-1
CRA-026440 hydrochloride
1H-Indole-2-carboxamide, 5-[2-(dimethylamino)ethoxy]-N-[3-[4-[(hydroxyamino)carbonyl]phenyl]-2-propyn-1-yl]-, hydrochloride (1:1) | [Molecular Formula]
C23H25ClN4O4 | [MOL File]
847459-98-7.mol | [Molecular Weight]
456.93 |
| Hazard Information | Back Directory | [Uses]
CRA-026440 hydrochloride is a potent, broad-spectrum HDAC (HDAC) inhibitor. The Ki values against recombinant HDAC isoenzymes HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, and HDAC10 are 4 nM, 14 nM, 11 nM, 15 nM, 7 nM, and 20 nM respectively. CRA-026440 hydrochloride shows antitumor and antiangiogenic activities[1]. CRA-026440 (hydrochloride) 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 hydrochloride (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 (IC50); HDAC2: 14 nM (IC50); HDAC3/SMRT: 11 nM (IC50); HDAC6: 15 nM (IC50); HDAC8: 7 nM (IC50); HDAC10: 20 nM (IC50) | [References]
[1] [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 |
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