Spiclomazine hydrochloride (APY-606) 是一种抗精神病药和抗肿瘤药。Spiclomazine hydrochloride 抑制KRas。Spiclomazine hydrochloride 诱导癌细胞凋亡(apoptosis)。
| 生物活性 | Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibitsKRas. Spiclomazine hydrochloride inducescancercellapoptosis[1][2]. |
| IC50& Target[2] | |
体外研究
(In Vitro) | Spiclomazine (0-100 μg/mL; 24 and 48 h) hydrochloride 以剂量依赖的方式抑制胰腺癌细胞的非接触集落形成[1]。
Spiclomazine (0.5x and 1x IC50; 48 h) hydrochloride 通过线粒体途径诱导 CFPAC-1 和 MIA PaCa-2 细胞凋亡，显著提高细胞内 ROS 水平[1]。
Spiclomazine (30 μg/mL; 24 h) hydrochloride 抑制 CFPAC-1 和 MIA PaCa-2 细胞的细胞运动性[1]。
Spiclomazine (10 and 20 μg/mL; 24 h) hydrochloride 在 G2 期时阻滞癌细胞周期进展[2]。
Cell Viability Assay[1] | Cell Line: | CFPAC-1, MIA PaCa-2, HEK-293 and HL-7702 cells | | Concentration: | 0-100 μg/mL | | Incubation Time: | 24 and 48 h | | Result: | Resulted in a time and dose-dependent growth reduction of CFPAC-1 and MIA PaCa-2 cells. Exhibited less cytotoxicity to normal HEK-293 and HL-7702 cells. The IC50for 48 h treatment was 15.2±2.0 μg/mL (31.5±2.0 μM) for CFPAC-1, 12.9±0.9 μg/mL (26.8±0.9 μM) for MIA PaCa-2, 41.9±1.4 μg/mL (86.9±1.4 μM) for HEK-293, and 71.2±3.3 μg/mL (147.7±3.3 μM) for HL-7702, respectively. |
Apoptosis Analysis[1] | Cell Line: | CFPAC-1 and MIA PaCa-2 cells | | Concentration: | 7.6 and 15.2 μg/mL for CFPAC-1, 6.45 and 12.9 μg/mL for MIA PaCa-2 | | Incubation Time: | 48 h | | Result: | Increased early apoptotic cells. |
Western Blot Analysis[1] | Cell Line: | CFPAC-1 and MIA PaCa-2 cells | | Concentration: | 10, 20 and 30 μg/mL | | Incubation Time: | 24 h | | Result: | The cleavages of caspase-3/9 were increased in a dose-dependent manner. The expression of Bax was up-regulated concomitant with the related attenuation of Bcl-2 protein expression. The level of cytochrome c in cytosol was increased accompanied by the decrease of the level of cytochrome c in mitochondria. |
Cell Migration Assay[1] | Cell Line: | CFPAC-1 and MIA PaCa-2 cells | | Concentration: | 30 μg/mL | | Incubation Time: | 24 h | | Result: | Markedly suppressed the migration of both pancreatic carcinoma cells. |
Cell Invasion Assay[1] | Cell Line: | CFPAC-1 and MIA PaCa-2 cells | | Concentration: | 30 μg/mL | | Incubation Time: | 24 h | | Result: | Suppressed the invasion by down-regulating the expression of MMP-2/9. |
Cell Cycle Analysis[2] | Cell Line: | MIA PaCa-2, CFPAC-1, BxPC-3, Capan-1 and SW1990 cells | | Concentration: | 10 and 20 μg/mL | | Incubation Time: | 24 h | | Result: | Promoted cancer cell cycle arrest at either G2 phase in MIA PaCa-2, CFPAC-1, and BxPC-3 cell lines or S phase in Capan-1 and SW1990 cell lines. |
|
体内研究
(In Vivo) | Spiclomazine (68 mg/kg; i.p.; every other day for two weeks) hydrochloride 降低小鼠 MIA PaCa-2 异种移植肿瘤的生长[2]。
| Animal Model: | BALB/c mice, MIA PaCa-2 xenograft model[2] | | Dosage: | 68 mg/kg | | Administration: | Intraperitoneal injection, every other day for two weeks | | Result: | Completely blocked the growth of tumors in three of the five mice. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com