27007-85-8
27007-85-8 structure
- Name: 1-Thia-4,8-diazaspiro[4.5]decan-3-one,8-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]-, hydrochloride (1:1)
- Chemical Name: 8-[3-(2-chlorophenothiazin-10-yl)propyl]-1-thia-4,8-diazaspiro[4.5]decan-3-one,hydrochloride
- CAS Number: 27007-85-8
- Molecular Formula: C22H25Cl2N3OS2
- Molecular Weight: 482.48900
- Catalog: Signaling Pathways GPCR/G Protein Ras
- Create Date: 2017-11-18 20:42:02
- Modify Date: 2024-01-08 18:53:34
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Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibits KRas. Spiclomazine hydrochloride induces cancer cell apoptosis[1][2].
| Name | 8-[3-(2-chlorophenothiazin-10-yl)propyl]-1-thia-4,8-diazaspiro[4.5]decan-3-one,hydrochloride |
|---|---|
| Synonyms |
Disepron
APY-606 Clospirazine hydrochloride Spiclomazine hydrochloride Spiclomazine Diceplon 1-Thia-4,8-diazaspiro(4.5)decan-3-one,8-(3-(2-chlorophenothiazin-10-yl)propyl)-,hydrochloride 8-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]-1-thia-4,8-diazaspiro[4.5]decan-3-one hydrochloride |
| Description | Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibits KRas. Spiclomazine hydrochloride induces cancer cell apoptosis[1][2]. |
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| Related Catalog | |
| Target |
K-RAS |
| 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 IC50 for 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. |
| 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. |
| References |
| Density | 1.42g/cm3 |
|---|---|
| Boiling Point | 695.3ºC at 760mmHg |
| Molecular Formula | C22H25Cl2N3OS2 |
| Molecular Weight | 482.48900 |
| Flash Point | 374.3ºC |
| Exact Mass | 481.08200 |
| PSA | 86.18000 |
| LogP | 6.12160 |
| Vapour Pressure | 3.51E-19mmHg at 25°C |
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