UPGL00004 is a potent allosteric glutaminase C (GAC) inhibitor (IC50=29 nM; Kd=27 nM). UPGL00004 strongly inhibits the proliferation of highly aggressive triple-negative breast cancer cell lines.

Product information

CAS Number: 1890169-95-5

Molecular Weight: 534.66

Formula: C25H26N8O2S2

Chemical Name: 2-phenyl-N-[5-(4-{[5-(2-phenylacetamido)-1,3,4-thiadiazol-2-yl]amino}piperidin-1-yl)-1,3,4-thiadiazol-2-yl]acetamide

Smiles: O=C(CC1C=CC=CC=1)NC1=NN=C(S1)N1CCC(CC1)NC1=NN=C(NC(=O)CC2C=CC=CC=2)S1

InChiKey: MRYCNTHLPRENBA-UHFFFAOYSA-N

InChi: InChI=1S/C25H26N8O2S2/c34-20(15-17-7-3-1-4-8-17)27-23-30-29-22(36-23)26-19-11-13-33(14-12-19)25-32-31-24(37-25)28-21(35)16-18-9-5-2-6-10-18/h1-10,19H,11-16H2,(H,26,29)(H,27,30,34)(H,28,31,35)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 125 mg/mL (233.79 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

UPGL00004 inhibits MDA-MB-231, HS578T and TSE cells with IC50s of 70, 129, and 262 nM, respectively.

In Vivo:

The combination of UPGL00004 (1 mg/kg body weight) and Bevacizumab (2.5 mg/kg body weight) via intraperitoneal injection completely prevent any detectable increase in tumor size in a triple-negative breast cancer patient-derived tumor graft model.

Products are for research use only. Not for human use.