Home PI3K/Akt/mTOR PI3K inhibitor GO-203 TFA

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GO-203 TFA MUC1-C Inhibitor

Cat.No.S8674

GO-203 is a D-amino acid cell-penetrating peptide inhibitor of MUC1-C dimerization and thereby its oncogenic function.
GO-203 TFA PI3K inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 2426.77

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Quality Control

Batch: S867401 Water]100 mg/mL]false]]]false]]]false Purity: 99.77%
99.77

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In vitro
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Water : 100 mg/mL

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Chemical Information, Storage & Stability

Molecular Weight 2426.77 Formula

C87H170N52O19S2.C2HF3O2

 Storage (From the date of receipt)
CAS No. 1222186-26-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C(CCN)CC(C(=O)NC(CC(=O)N)C(=O)O)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CS)NC(=O)C(CCC(=O)N)NC(=O)C(CS)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)NC(=O)C(CCCNC(=N)N)N.C(=O)(C(F)(F)F)O

Mechanism of Action

Targets/IC50/Ki
MUC-1C
In vitro
GO-203 inhibits MUC1-C homodimerization which blocks its oncogenic function. Treatment of MUC1-overexpressing SKCO-1 and Colo-205 colon cancer cells with this compound is associated with downregulation of the TP53-inducible glycolysis and apoptosis regulator (TIGAR) protein. This chemical regulates AKT-S6K1-elF4A signaling in colorectal cancer cells. Targeting MUC1-C with it inhibits p-AKT in colorectal cancer cells. This treatment also results in increases in reactive oxygen species (ROS) and loss of mitochondrial transmembrane potential.
In vivo
GO-203 is effective in inhibiting growth and survival of MUC1-positive colorectal cancer cells in mouse xenograft models. It is also effective in xenografts models of breast, prostate, lung and certain hematologic malignancy.
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02204085 Active not recruiting
Acute Myeloid Leukemia in Relapse|Recurrent Adult Acute Myeloid Leukemia
Beth Israel Deaconess Medical Center|Dana-Farber Cancer Institute
 September 2014 Phase 1|Phase 2

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