847459-98-7
847459-98-7 structure
- Name: CRA-026440 hydrochloride
- Chemical Name: CRA-026440 hydrochloride
- CAS Number: 847459-98-7
- Molecular Formula: C23H25ClN4O4
- Molecular Weight: 456.92
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2023-01-14 18:29:17
- Modify Date: 2024-01-12 17:21:27
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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].
| Name | CRA-026440 hydrochloride |
|---|
| Description | 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]. |
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| Related Catalog | |
| Target |
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) |
| In Vitro | CRA-026440 hydrochloride 对 HUVEC 内皮细胞具有抗增殖作用，GI50 值为 1.41 μM[1]。 CRA-026440 hydrochloride（0.1-10 μM；18 小时）导致乙酰化组蛋白和乙酰化微管蛋白的积累，从而抑制肿瘤细胞生长并诱导细胞凋亡[1]。 CRA-026440 hydrochloride（0.1-10 μM；5 天）以剂量依赖性方式抑制离体血管生成[1]。 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；静脉注射；每天；连续三天）导致携带 HCT116 或 U937 人肿瘤异种移植物的小鼠肿瘤生长显着减少[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. |
| References |
| Molecular Formula | C23H25ClN4O4 |
|---|---|
| Molecular Weight | 456.92 |