1063714-11-3

1063714-11-3 structure

Name: CXL017
Chemical Name: Ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
CAS Number: 1063714-11-3
Molecular Formula: C₂₄H₂₇NO₇
Molecular Weight: 441.474
Create Date: 2020-01-11 13:49:49
Modify Date: 2024-01-03 07:46:09
CXL017 is a small molecule that has selective cytotoxicity toward MDR cancer cell lines in vitro, through inhibition of the sarco/endoplasmic reticulum Ca(2+)-ATPase (SERCA) with IC50 of 15 uM; selectively suppresses the growth of tumors derived from the MDR cancer cell line, HL60/MX2, in vivo; significantly downregulates Mcl-1 and Bax and up-regulates Noxa, Bim, Bcl-XL, SERCA2, and SERCA3 proteins, along with a reduction in endoplasmic reticulum (ER) calcium content in HL60/MX2 cells; elicits its cytotoxic effect, in part, through inhibition of the SERCA.

Name	Ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate
Synonyms	Ethyl 2-amino-6-(3,5-dimethoxyphenyl)-4-(2-ethoxy-2-oxoethyl)-4H-chromene-3-carboxylate 4H-1-Benzopyran-4-acetic acid, 2-amino-6-(3,5-dimethoxyphenyl)-3-(ethoxycarbonyl)-, ethyl ester

Description	CXL017 is a small molecule that has selective cytotoxicity toward MDR cancer cell lines in vitro, through inhibition of the sarco/endoplasmic reticulum Ca(2+)-ATPase (SERCA) with IC50 of 15 uM; selectively suppresses the growth of tumors derived from the MDR cancer cell line, HL60/MX2, in vivo; significantly downregulates Mcl-1 and Bax and up-regulates Noxa, Bim, Bcl-XL, SERCA2, and SERCA3 proteins, along with a reduction in endoplasmic reticulum (ER) calcium content in HL60/MX2 cells; elicits its cytotoxic effect, in part, through inhibition of the SERCA.
References	References 1. Das SG, et al. ACS Chem Biol. 2013 Feb 15;8(2):327-35. 2. Aridoss G, et al. J Med Chem. 2012 Jun 14;55(11):5566-81. 3. Hermanson DL, et al. Mol Pharmacol. 2013 Aug;84(2):236-43. 4. Bleeker NP, et al. Mol Pharm. 2013 Nov 4;10(11):4358-66. View Related Products by Target Other Targets