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GO-203 TFA is a potent MUC1-C oncoprotein inhibitor. GO-203 TFA is an all D-amino acid peptide that consists of a poly-R transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. GO-203 TFA downregulates TIGAR (TP53-induced glycolysis and apoptosis regulator) protein synthesis by inhibiting the PI3K-AKT-S6K1 pathway. GO-203 TFA induces the production of ROS and loss of mitochondrial transmembrane potential. GO-203 TFA inhibits the growth of colon cancer cells in vitro and as xenografts in nude mice[1][2]. | [in vivo]
GO-203 (18 mg/kg/day; IP; for 28 days) TFA significantly inhibits growth of the COLO-205 tumors[2].
| Animal Model: | Four- to 6-week-old BALB/c nu/nu male/female mice with Colo-205 or SKCO-1 cells[2] | | Dosage: | 18 mg/kg | | Administration: | IP; daily; for 28 days | | Result: | Significantly inhibited growth of the COLO-205 tumors.
These tumors regressed completely by the end of treatment (day 28) and there was no evidence for regrowth by day 180.
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PI3K | [References]
[1] Masanori Hasegawa, et al. Intracellular Targeting of the Oncogenic MUC1-C Protein with a Novel GO-203 Nanoparticle Formulation. Clin Cancer Res. 2015 May 15;21(10):2338-47. DOI:10.1158/1078-0432.CCR-14-3000
[2] Rehan Ahmad, et al. Targeting MUC1-C inhibits the AKT-S6K1-elF4A pathway regulating TIGAR translation in colorectal cancer. Mol Cancer. 2017 Feb 2;16(1):33. DOI:10.1186/s12943-017-0608-9 |
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