[CAS NO. 847459-98-7] CRA-026440 hydrochloride
PRODUCTS SPECIFICATIONS [847459-98-7]
DESCRIPTION [847459-98-7]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 456.92 |
| Molecular Formula | C23H25ClN4O4 |
| SMILES | O=C(C(N1)=CC2=C1C=CC(OCCN(C)C)=C2)NCC#CC3=CC=C(C(NO)=O)C=C3.[H]Cl |
Summary
CRA-026440 hydrochloride is a potent, broad-spectrum HDAC ( HDAC ) inhibitor. The K i 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] .
IC50 & Target
|
HDAC1 4 nM (IC 50 ) |
HDAC2 14 nM (IC 50 ) |
HDAC3/SMRT 11 nM (IC 50 ) |
HDAC6 15 nM (IC 50 ) |
HDAC8 7 nM (IC 50 ) |
HDAC10 20 nM (IC 50 ) |
In Vitro
CRA-026440 hydrochloride has antiproliferative effect on HUVEC endothelial cells with a GI
50
value of 1.41 μM
[1]
.
CRA-026440 hydrochloride (0.1-10 μM; 18 hours) results in the accumulation of acetylated histone and acetylated tubulin, leading to an inhibition of tumor cell growth and the induction of apoptosis
[1]
.
CRA-026440 hydrochloride (0.1-10 μM; 5 days) inhibits ex vivo angiogenesis in a dose-dependent manner
[1]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis [1]
| Cell Line: | HCT116 cells |
| Concentration: | 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM |
| Incubation Time: | 18 hours |
| Result: | Resulted in the accumulation of both acetylated histones and acetylated tubulin. Induced expression of the cyclin-dependent kinase inhibitor p21Cip1/WAF1. |
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |