| Identification | Back Directory | [Name]
CYD-2-11 | [CAS]
1425944-22-4 | [Synonyms]
CYD-2-11
CYD-2-11 TFA salt
Ethanamine, 2-[2-[(2-nitro-9H-fluoren-9-ylidene)methyl]phenoxy]- | [Molecular Formula]
C22H18N2O3 | [MOL File]
1425944-22-4.mol | [Molecular Weight]
358.39 |
| Hazard Information | Back Directory | [Description]
CYD-2-11 is a potent and selective Bax agonist. It acts by targeting the structural pocket proximal to S184 in the C-terminal region of Bax. | [Uses]
CYD-2-11 is a selective Bax agonist with a Ki value of 34.1 nM. CYD-2-11 induces cell apoptosis and shows antiproliferative activity to breast cancer MDA-MB-231 and MCF-7 cell lines with IC50 values of 3.22 and 3.81 μM, respectively. CYD-2-11 suppresses tumor growth in MDA-MB-231 tumor models. CYD-2-11 can be used for the research of breast and lung cancer[1][2]. | [in vivo]
CYD-2-11 (20 mg/kg; i.p.; once daily for 7 days) inhibits tumor growth[1].
CYD-2-11 (40 mg/kg; i.p.; once daily for 14 days) represses lung cancer growth and overcomes rapalog resistance with the combination of RAD001 (1 mg/kg) in murine lung cancer models[2]. | Animal Model: | Female nude mice with MDA-MB-231 tumor xenografts[1] | | Dosage: | 20 mg/kg | | Administration: | Intraperitoneal injection; 20 mg/kg; once daily for 7 days | | Result: | Exhibited a 57% inhibition rate of MDA-MB-231 tumor growth in vivo.
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| [References]
[1] Liu G, et al. Structure-activity relationship studies on Bax activator SMBA1 for the treatment of ER-positive and triple-negative breast cancer. Eur J Med Chem. 2019 Sep 15;178:589-605. DOI:10.1016/j.ejmech.2019.06.004
[2] Li R, et al. Modulation of Bax and mTOR for Cancer Therapeutics. Cancer Res. 2017 Jun 1;77(11):3001-3012. doi: 10.1158/0008-5472.CAN-16-2356. Epub 2017 Apr 5. DOI:10.1158/0008-5472.CAN-16-2356 |
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