CXL017

Names

[ Name ]:
CXL017

[Synonym ]:
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

Biological Activity

[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

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
571.4±50.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₄H₂₇NO₇

[ Molecular Weight ]:
441.474

[ Flash Point ]:
188.6±26.4 °C

[ Exact Mass ]:
441.178741

[ LogP ]:
3.79

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.553

Related Compounds

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