| Identification | Back Directory | [Name]
Spiclomazine | [CAS]
27007-85-8 | [Synonyms]
Apy 606 Diceplon Disepron Nsc290956 Spiclomazine HCl Spiclomazine Hydrochloride Clospirazine hydrochloride 1-Thia-4,8-diazaspiro[4.5]decan-3-one, 8-[3-(2-chlorophenothiazin-10-yl)propyl]-, monohydrochloride 1-Thia-4,8-diazaspiro[4.5]decan-3-one, 8-[3-(2-chloro-10H-phenothiazin-10-yl)propyl]-, monohydrochloride | [Molecular Formula]
C22H25Cl2N3OS2 | [MDL Number]
MFCD01681961 | [MOL File]
27007-85-8.mol | [Molecular Weight]
482.48 |
| Hazard Information | Back Directory | [Uses]
Spiclomazine hydrochloride (APY-606) is an antipsychotic and antitumor agent. Spiclomazine hydrochloride inhibits KRas. Spiclomazine hydrochloride induces cancer cell apoptosis[1][2]. | [Definition]
ChEBI: Clospirazine hydrochloride is a member of phenothiazines. | [in vivo]
Spiclomazine (68 mg/kg; i.p.; every other day for two weeks) hydrochloride reduces the growth of MIA PaCa-2 xenograft in mice[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. |
| [IC 50]
K-RAS | [References]
[1] Zhao W, et al. Spiclomazine induces apoptosis associated with the suppression of cell viability, migration and invasion in pancreatic carcinoma cells. PLoS One. 2013 Jun 20;8(6):e66362. DOI:10.1371/journal.pone.0066362 [2] Guo X, et al. Spiclomazine displays a preferential anti-tumor activity in mutant KRas-driven pancreatic cancer. Oncotarget. 2018 Jan 8;9(6):6938-6951. DOI:10.18632/oncotarget.24025 |
| Safety Data | Back Directory | [Toxicity]
LD50 in mice, rats (mg/kg): 3400, 2950 i.p.; >5490, >5490 s.c.; 3800, 4000 orally (Nakanishi, 1970) |
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