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Chemical Structure| 1222186-26-6 Chemical Structure| 1222186-26-6

Structure of GO-203 TFA
CAS No.: 1222186-26-6

Chemical Structure| 1222186-26-6

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GO-203 TFA is an inhibitor of MUC1-C oncogenic protein, effectively inducing apoptosis in cancer cells by downregulating TIGAR protein synthesis.

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Product Details of GO-203 TFA

CAS No. :1222186-26-6
Formula : C89H171F3N52O21S2
M.W : 2426.77
SMILES Code : C(C(O)=O)(F)(F)F.[C@@H](C(N[C@@H](C(N[C@@H](C(N[C@@H](C(N[C@@H](C(N[C@@H](C(N[C@@H](C(N[C@@H](C(N[C@@H](C(N[C@@H](C(N[C@H](CC(N)=O)C(O)=O)=O)CCCCN)=O)CCCNC(=N)N)=O)CCCNC(=N)N)=O)CS)=O)CCC(N)=O)=O)CS)=O)CCCNC(=N)N)=O)CCCNC(=N)N)=O)CCCNC(=N)N)=O)(NC([C@H](NC([C@H](NC([C@H](NC([C@H](NC([C@@H](CCCNC(=N)N)N)=O)CCCNC(=N)N)=O)CCCNC(=N)N)=O)CCCNC(=N)N)=O)CCCNC(=N)N)=O)CCCNC(=N)N
MDL No. :N/A
InChI Key :WIUOAIBLROIIFP-BHDSHVNUSA-N
Pubchem ID :137967120

Safety of GO-203 TFA

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319
Precautionary Statements:P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
LOVO cells 5 μM 6 days GO-203 has no effect on MUC1-negative cells Mol Cancer. 2017 Feb 2;16(1):33
SW480 cells 5 μM 6 days GO-203 has no effect on MUC1-negative cells Mol Cancer. 2017 Feb 2;16(1):33
COLO-205 cells 5 μM 6 days GO-203 inhibits cell growth Mol Cancer. 2017 Feb 2;16(1):33
SKCO-1 cells 5 μM 3 days GO-203 inhibits AKT-mTORC-S6K1 signaling pathway Mol Cancer. 2017 Feb 2;16(1):33
H460 cells 5 μM 48 hours Inhibition of MUC1-C led to downregulation of MYC expression Cancer Res. 2016 Mar 15;76(6):1538-48
A549 cells 5 μM 48 hours Inhibition of MUC1-C led to downregulation of MYC expression Cancer Res. 2016 Mar 15;76(6):1538-48
HCT116 cells 5 μM 3 days Induced MICA/B expression, inhibited exosome secretion J Immunother Cancer. 2023 Feb;11(2):e006238
4T1 cells 2.5 μM 5 days To evaluate the effect of GO-203 on MUC1-C and SOD enzyme levels, results showed that GO-203 treatment reduced the expression of MUC1-C and SOD enzymes. Nat Commun. 2024 Sep 28;15(1):8416
MDA-MB-231 cells 2.5 μM 5 days To evaluate the effect of GO-203 on MUC1-C and SOD enzyme levels, results showed that GO-203 treatment reduced the expression of MUC1-C and SOD enzymes. Nat Commun. 2024 Sep 28;15(1):8416
SUM149 TNBC cells 1 μM 48 hours Inhibits MUC1-C nuclear localization, induces γH2AX, and enhances CDDP-induced DNA damage and cell death Cancer Res. 2019 Apr 15;79(8):2031-2041
BT-549 TNBC cells 1 μM 48 hours Inhibits MUC1-C nuclear localization, induces γH2AX, and enhances CDDP-induced DNA damage and cell death Cancer Res. 2019 Apr 15;79(8):2031-2041
BT-549 cells 5 μM 3 days Induced MICA/B expression, inhibited exosome secretion J Immunother Cancer. 2023 Feb;11(2):e006238
COLO 201 cells 5 μM 3 days Induced MICA/B expression, inhibited exosome secretion J Immunother Cancer. 2023 Feb;11(2):e006238
RKO cells 5 μM 3 days Induced MICA/B expression, inhibited exosome secretion J Immunother Cancer. 2023 Feb;11(2):e006238
LLC/MUC1 cells 2.5 μM 72 hours To evaluate the effect of GO-203 on MUC1-C and PD-L1 expression, results showed that GO-203 treatment downregulated MUC1-C and PD-L1 and induced IFN-γ expression. Oncoimmunology. 2017 Jul 5;6(9):e1338998
H660 NEPC cells 2 μM 24 hours GO-203 treatment decreased H660 cell survival and induced ferroptosis, as evidenced by lipid peroxidation and increased TfR1 expression. Cell Death Discov. 2024 Jan 5;10(1):9
DU-145 CRPC cells 2 μM 24 hours GO-203 treatment decreased DU-145 cell survival and induced ferroptosis, as evidenced by lipid peroxidation and increased TfR1 expression. Cell Death Discov. 2024 Jan 5;10(1):9
Myla cells 3 μM 3 days Combination of GO-203 with decitabine significantly increased ROS levels, leading to apoptosis Mol Cancer Ther. 2017 Oct;16(10):2304-2314
HuT-78 cells 3 μM 3 days Combination of GO-203 with decitabine significantly increased ROS levels, leading to apoptosis Mol Cancer Ther. 2017 Oct;16(10):2304-2314
H9 cells 3 μM 3 days Combination of GO-203 with decitabine significantly increased ROS levels, leading to apoptosis Mol Cancer Ther. 2017 Oct;16(10):2304-2314
RPMI8226 cells 2.5 μM 72 hours Evaluate the effect of GO-203 combined with LEN on downregulation of β-catenin and MYC, showing that the combination is more effective than either agent alone. Br J Haematol. 2017 Sep;178(6):914-926
MM.1S cells 2.5 μM 72 hours Evaluate the effect of GO-203 combined with LEN on downregulation of β-catenin and MYC, showing that the combination is more effective than either agent alone. Br J Haematol. 2017 Sep;178(6):914-926

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice COLO-205 and SKCO-1 colon cancer xenograft models Intraperitoneal or intravenous injection 18 mg/kg or 6 mg/kg or 3 mg/kg Once daily for 28 days or 5 days GO-203 significantly inhibited tumor growth and resulted in complete tumor regression Mol Cancer. 2017 Feb 2;16(1):33
NSG mice Breast cancer model Intravenous injection 4 mg/kg 5 consecutive days To evaluate the effect of GO-203 on ROS levels in GFP+ CTCs, results showed that GO-203 treatment significantly increased ROS levels in GFP+ CTCs. Nat Commun. 2024 Sep 28;15(1):8416
Nude mice SUM149 TNBC xenograft model Intraperitoneal injection 15 mpk Once a week for three weeks Combination of GO-203/NPs and olaparib significantly inhibits tumor growth Cancer Res. 2019 Apr 15;79(8):2031-2041
NCR nu/nu mice H460 tumor xenograft model Intraperitoneal injection 12 mg/kg Daily administration until tumor volume reached ~150 mm3 Combination of GO-203 and JQ1 significantly inhibited tumor growth and downregulated MYC levels Cancer Res. 2016 Mar 15;76(6):1538-48
MUC1 transgenic mice LLC/MUC1 tumor model Intraperitoneal injection 15 mg/kg Once a week for 2 weeks To evaluate the effect of GO-203 on the tumor microenvironment, results showed that GO-203 treatment inhibited tumor growth, downregulated PD-L1 expression, and enhanced the effector function of CD8+ T cells. Oncoimmunology. 2017 Jul 5;6(9):e1338998
NSG mice H9 cell xenograft model Intradermal injection 14 mg/kg Once daily for 3 weeks Combination of GO-203 with decitabine significantly inhibited tumor growth and increased apoptotic cells Mol Cancer Ther. 2017 Oct;16(10):2304-2314

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

0.41mL

0.08mL

0.04mL

2.06mL

0.41mL

0.21mL

4.12mL

0.82mL

0.41mL

 

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