GO-203
GO-203 Basic information
- Product Name:
- GO-203
- Synonyms:
-
- GO-203
- GO-203 TFA
- (6R,9R,12R,15R,18R,21R,24R,27R,30R,33S,36R,39S,42R,45R,48R,51R)-1,6-Diamino-51-(2-amino-2-oxoethyl)-36-(3-amino-3-oxopropyl)-48-(4-aminobutyl)-9,12,15,18,21,24,27,30,42,45-decakis(3-guanidinopropyl)-1-imino-33,39-bis(mercaptomethyl)-7,10,13,16,19,22,25,28,31,34,37,40,43,46,49-pentadecaoxo-2,8,11,14,17,20,23,26,29,32,35,38,41,44,47,50-hexadecaazadopentacontan-52-oic acid 2,2,2-trifluoroacetic acid salt
- CAS:
- 1222186-26-6
- MF:
- C89H171F3N52O21S2
- MW:
- 2426.81
- Mol File:
- 1222186-26-6.mol
GO-203 Chemical Properties
- form
- Solid
- color
- White to off-white
- Sequence
- d-{Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Arg-Cys-Gln-Cys-Arg-Arg-Lys-Asn} (TFA salt)
GO-203 Usage And Synthesis
Uses
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. |
IC 50
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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