PACMA31

Names

[ Name ]:
PACMA31

[Synonym ]:
MFCD26793891
Ethyl N-{[(2,4-dimethoxyphenyl)(propioloyl)amino](2-thienyl)acetyl}glycinate
Glycine, N-[2-[(2,4-dimethoxyphenyl)(1-oxo-2-propyn-1-yl)amino]-2-(2-thienyl)acetyl]-, ethyl ester
PACMA 31
N-(2,4-Dimethoxyphenyl)-N-(1-oxo-2-propyn-1-yl)-2-(2-thienyl)glycyl-glycine ethyl ester

Biological Activity

[Description]:

An orally active, irreversible inhibitor of protein disulfide isomerase (PDI), forming a covalent bond with the active site cysteines of PDI; significantly inhibits human ovarian cancer cells OVCAR-8, HEY, and OVCAR-8 growth with IC50 of 0.9, 1.4, and 0.32 uM; significantly suppresses ovarian tumor growth without causing toxicity to normal tissues in mouse xenograft model of human OVCAR-8 ovarian cancer.

[References]

References 1. Xu S, et al. Proc Natl Acad Sci U S A. 2012 Oct 2;109(40):16348-53. 2. Vatolin S, et al. Cancer Res. 2016 Jun 1;76(11):3340-50. View Related Products by Target Protein Disulfide Isomerase (PDI)

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C₂₁H₂₂N₂O₆S

[ Molecular Weight ]:
430.474

[ Exact Mass ]:
430.119843

[ LogP ]:
1.50

[ Index of Refraction ]:
1.592

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ RIDADR ]:
UN 2811 6.1 / PGIII

Related Compounds

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