Description
GL0388 is a Bax activator that results in Bax insertion into mitochondrial membrane. GL0388 shows antiproliferative activities against various cancer cells, with IC50s of 0.299-1.57 μM. GL0388 activates Bax and induce Bax-mediated apoptosis. GL0388 suppresses breast cancer xenograft tumor growth in vivo.
Product information
Molecular Weight: 332.37
Formula: C21H17FN2O
Chemical Name: (E)-2-((3-((2-fluoro-9H-fluoren-9-ylidene)methyl)pyridin-2-yl)oxy)ethan-1-amine
Smiles: NCCOC1=NC=CC=C1/C=C1/C2=CC(F)=CC=C2C2=CC=CC=C/12
InChiKey: WCVGRSPKTHQNCR-XDHOZWIPSA-N
InChi: InChI=1S/C21H17FN2O/c22-15-7-8-18-16-5-1-2-6-17(16)19(20(18)13-15)12-14-4-3-10-24-21(14)25-11-9-23/h1-8,10,12-13H,9,11,23H2/b19-12+
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
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:
GL0388 (0.1-10 μM; 72 h) inhibits the cell proliferation of MDA-MB-231 and MCF-7 breast cancer cell lines, with IC50s of 0.96 μM and 0.52 μM, respectively. GL0388 (0.01-100 μM) inhibits the cell proliferation in 60 human tumor cell lines, with GI550s of 0.299-1.57 μM. GL0388 (1-10 μM; 48 h) significantly upregulates the cleaved PARP-1 and cleaved caspase 3 in MDA-MB-231 cells. GL0388 (0.1-1 μM; 24 h) inhibits the colony formation and invasion of breast cancer cells. GL0388 (1-10 μM; 24 h) promotes Bax insertion into mitochondrial membranes of MDA-MB-231 cells in a dose-dependent manner. GL0388 increases cytochrome c in the cytosolic fraction of MDA-MB-231 cells.
In Vivo:
GL0388 (10-20 mg/kg for i.p.; 15 mg/kg for i.t.; once daily for 10 days) dose-dependently suppresses the growth of MDA-MB-231 tumors in mice.
Products are for research use only. Not for human use.
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