| Identification | Back Directory | [Name]
CYSMETHYNIL | [CAS]
851636-83-4 | [Synonyms]
CYSMETHYNIL
2-[5-(3-methylphenyl)-1-octylindol-3-yl]acetamide
1H-Indole-3-acetamide, 5-(3-methylphenyl)-1-octyl- | [Molecular Formula]
C25H32N2O | [MDL Number]
MFCD22572757 | [MOL File]
851636-83-4.mol | [Molecular Weight]
376.53 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMF: 3.3 mg/ml; DMSO: 5 mg/ml; Ethanol: 20 mg/ml | [form ]
A crystalline solid | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Uses]
Cysmethynil is an Icmt inhibitor(IC50 = 2.4 μM). Cysmethynil inhibites RAS membrane binding and EGF signal transduction. Cysmethynil prevents the cells in the G1 phase and induces autophagy. Cysmethynil inhibits PC3 cells proliferation, has synergistic effect with Paclitaxel (HY-B0015) and Doxorubicin (HY-15142A). Cysmethynil has anti-tumor effects and can be used for solid tumor (such as prostate cancer et al.) research[1][2][3]. | [in vivo]
Cysmethynil (100 mg/kg, 200 mg/kg; intraperitoneal injection; every 48 h; 28 day) without adverse effects on mice body weight, significantly impacts on tumor growth, causes both an accumulation of cells in the G1 phase and cell death [2].
Cysmethynil (20 mg/kg; intraperitoneal injection; three times a week; 2 weeks; alone or combined with Paclitaxel? (HY-B0015)/ Doxorubicin (HY-15142A) ) is not toxic to mice and induces only moderate inhibition of tumor growth as single agent, the combination with Paclitaxel(HY-B0015)/ Doxorubicin(HY-15142A) results in significantly greater efficacy in inhibiting tumor growth. Cysmethynil sensitizes cervical cancer cells to chemotherapy agent in xenograft mouse model[3].
| Animal Model: | 6 week-old SCID mice with SiHa cells in the mice flank [3] | | Dosage: | 20 mg/kg (single; combination with Paclitaxel or Doxorubicin) | | Administration: | intraperitoneal injection; three times a week; 2 weeks | | Result: | Decreased in tumor size when treated with Cys alone, or Cysmethynil+Paclitaxel(HY-B0015)/Cysmethynil+ Doxorubicin(HY-15142A) . |
| Animal Model: | SCID mice with PC3 cells in a xenograft model[2] | | Dosage: | 0.1 mg/g or 0.2 mg/g Cysmethynil | | Administration: | intraperitoneal injection; every 48 h; 28 days | | Result: | Decreased in tumor size when treated with both doses of cysmethynil. |
| [storage]
Store at -20°C | [References]
[1] Winter-Vann AM, et al. A small-molecule inhibitor of isoprenylcysteine carboxyl methyltransferase with antitumor activity in cancer cells. Proc Natl Acad Sci U S A. 2005 Mar 22;102(12):4336-41. DOI:10.1073/pnas.0408107102
[2] Wang M, et al. A small molecule inhibitor of isoprenylcysteine carboxymethyltransferase induces autophagic cell death in PC3 prostate cancer cells. J Biol Chem. 2008 Jul 4;283(27):18678-84. DOI:10.1074/jbc.M801855200
[3] Pan Q, et al. Inhibition of isoprenylcysteine carboxylmethyltransferase sensitizes common chemotherapies in cervical cancer via Ras-dependent pathway. Biomed Pharmacother. 2018 Mar;99:169-175. DOI:10.1016/j.biopha.2018.01.048
[4] Zhu C, et al. Targeting KRAS mutant cancers: from druggable therapy to drug resistance. Mol Cancer. 2022 Aug 4;21(1):159. DOI:10.1186/s12943-022-01629-2 |
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