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| 5mg |
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| 10mg |
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| Targets |
GO-203 TFA targets the MUC1-C oncoprotein, a heterodimeric cell surface-associated protein that is overexpressed and aberrantly localized in various human cancers. The peptide's CQCRRKN motif binds to the MUC1-C cytoplasmic tail, blocking its homodimerization, which is essential for its oncogenic function. By inhibiting MUC1-C dimerization, GO-203 disrupts downstream signaling pathways that promote cancer cell growth, survival, and chemoresistance.
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| ln Vitro |
GO-203 TFA is an anti-cancer peptide that inhibits the MUC1-C oncoprotein, blocking its dimerization and oncogenic function. In preclinical studies, it has demonstrated the ability to target and disrupt cancer cell growth and survival. The peptide's all-D-amino acid composition provides resistance to proteolytic degradation, enhancing its stability and activity in biological systems. GO-203 TFA shows potential for targeting intracellular proteins involved in cancer progression.
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| ln Vivo |
In vivo, GO-203 TFA has shown potential in preclinical studies for targeting and disrupting cancer cell growth and survival. As a cell-penetrating peptide inhibitor of the MUC1-C oncoprotein, it is designed to block MUC1-C dimerization and inhibit its oncogenic functions in animal models of cancer. The compound's all-D-amino acid structure contributes to its stability and bioavailability in vivo. Specific in vivo efficacy data and detailed animal model studies are not extensively documented in the public domain.
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| Enzyme Assay |
The in vitro biochemical activity of GO-203 TFA is typically assessed using binding assays to confirm its interaction with the MUC1-C cytoplasmic tail. The peptide is incubated with recombinant MUC1-C protein or cell lysates containing MUC1-C at varying concentrations (typically 0.001-100 µM). Binding affinity is determined using techniques such as surface plasmon resonance (SPR) or co-immunoprecipitation followed by Western blot analysis. The inhibition of MUC1-C homodimerization can be assessed by crosslinking assays or native gel electrophoresis.
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| Cell Assay |
In vitro cellular assays for GO-203 TFA involve treating MUC1-expressing cancer cell lines with the peptide at concentrations ranging from 0.01 to 10 µM for 24-72 hours. Cellular viability is assessed using MTT, CCK-8, or CellTiter-Glo assays. The inhibition of MUC1-C dimerization and downstream signaling is evaluated by Western blot analysis of MUC1-C and its target proteins. Apoptosis is assessed by Annexin V/PI staining or caspase activity assays. The peptide is dissolved in DMSO or sterile water and diluted in cell culture medium.
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| Animal Protocol |
In vivo animal studies for GO-203 TFA typically involve administration to mice via intraperitoneal or intravenous injection at doses determined from preliminary studies. Tumor xenograft models using MUC1-expressing human cancer cell lines are used to evaluate antitumor efficacy. Tumor growth is monitored by caliper measurements. The peptide's effects on MUC1-C signaling, tumor proliferation, and apoptosis are assessed by immunohistochemistry and Western blot analysis of tumor tissues. The peptide is formulated in appropriate vehicles for administration.
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| ADME/Pharmacokinetics |
GO-203 TFA has a molecular weight of approximately 2426.77 g/mol and formula C89H171F3N52O21S2. It is a peptide composed entirely of D-amino acids, providing resistance to proteolytic degradation. The peptide is soluble in DMSO and sterile water. Recommended storage is powder at -20°C for up to 3 years and in solvent at -80°C for 6 months or -20°C for 1 month. Detailed PK parameters such as half-life, Cmax, AUC, and bioavailability would require experimental determination.
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| Toxicity/Toxicokinetics |
GO-203 TFA is intended for research use only and is not approved for human therapeutic applications. As a peptide-based inhibitor, it is generally considered to have a favorable safety profile, but appropriate safety precautions should be taken when handling. Standard preclinical toxicity assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, and assessment of off-target effects. The compound's all-D-amino acid composition may reduce immunogenicity compared to L-amino acid peptides.
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| References | |
| Additional Infomation |
GO-203 TFA (CAS 1222186-26-6) is a potent cell-penetrating peptide inhibitor of the MUC1-C oncoprotein, composed entirely of D-amino acids. It consists of a poly-arginine transduction domain linked to a CQCRRKN motif that binds to the MUC1-C cytoplasmic tail and blocks MUC1-C homodimerization. The peptide is designed for research in oncology, specifically for targeting MUC1-C-driven cancers. GO-203 TFA is also known by its peptide sequence H-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-D-Arg-D-Cys-D-Gln-D-Cys-D-Arg-D-Arg-D-Lys-D-Asn-OH.TFA.
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| Molecular Formula |
C89H171F3N52O21S2
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|---|---|
| Molecular Weight |
2426.7711
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| Exact Mass |
2425.33
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| CAS # |
1222186-26-6
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| Related CAS # |
L-GO-203 TFA
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| PubChem CID |
137967120
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
56
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| Hydrogen Bond Acceptor Count |
39
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| Rotatable Bond Count |
97
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| Heavy Atom Count |
167
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| Complexity |
4940
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| Defined Atom Stereocenter Count |
16
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| SMILES |
SC[C@H](C(N[C@@H](C(N[C@H](CS)C(N[C@@H](C(N[C@@H](C(N[C@@H](C(N[C@@H](C(=O)O)CC(N)=O)=O)CCCCN)=O)CCCNC(=N)N)=O)CCCNC(=N)N)=O)=O)CCC(N)=O)=O)NC([C@@H](CCCNC(=N)N)NC([C@@H](CCCNC(=N)N)NC([C@@H](CCCNC(=N)N)NC([C@@H](CCCNC(=N)N)NC([C@@H](CCCNC(=N)N)NC([C@@H](CCCNC(=N)N)NC([C@@H](CCCNC(=N)N)NC([C@@H](CCCNC(=N)N)NC([C@@H](CCCNC(=N)N)N)=O)=O)=O)=O)=O)=O)=O)=O)=O.FC(C(=O)O)(F)F
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| InChi Key |
WIUOAIBLROIIFP-BHDSHVNUSA-N
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| InChi Code |
InChI=1S/C87H170N52O19S2.C2HF3O2/c88-28-2-1-15-44(71(152)137-56(76(157)158)40-60(91)141)126-63(144)46(17-5-31-116-79(96)97)133-70(151)53(24-12-38-123-86(110)111)135-74(155)57(41-159)139-73(154)55(26-27-59(90)140)136-75(156)58(42-160)138-72(153)54(25-13-39-124-87(112)113)134-69(150)52(23-11-37-122-85(108)109)132-68(149)51(22-10-36-121-84(106)107)131-67(148)50(21-9-35-120-83(104)105)130-66(147)49(20-8-34-119-82(102)103)129-65(146)48(19-7-33-118-81(100)101)128-64(145)47(18-6-32-117-80(98)99)127-62(143)45(16-4-30-115-78(94)95)125-61(142)43(89)14-3-29-114-77(92)93;3-2(4,5)1(6)7/h43-58,159-160H,1-42,88-89H2,(H2,90,140)(H2,91,141)(H,125,142)(H,126,144)(H,127,143)(H,128,145)(H,129,146)(H,130,147)(H,131,148)(H,132,149)(H,133,151)(H,134,150)(H,135,155)(H,136,156)(H,137,152)(H,138,153)(H,139,154)(H,157,158)(H4,92,93,114)(H4,94,95,115)(H4,96,97,116)(H4,98,99,117)(H4,100,101,118)(H4,102,103,119)(H4,104,105,120)(H4,106,107,121)(H4,108,109,122)(H4,110,111,123)(H4,112,113,124);(H,6,7)/t43-,44-,45-,46-,47-,48-,49-,50-,51-,52-,53-,54-,55-,56-,57-,58-;/m1./s1
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| Chemical Name |
(2R)-4-amino-2-[[(2R)-6-amino-2-[[(2R)-2-[[(2R)-2-[[(2S)-2-[[(2R)-5-amino-2-[[(2S)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-[[(2R)-2-amino-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]-3-sulfanylpropanoyl]amino]-5-oxopentanoyl]amino]-3-sulfanylpropanoyl]amino]-5-carbamimidamidopentanoyl]amino]-5-carbamimidamidopentanoyl]amino]hexanoyl]amino]-4-oxobutanoic acid;2,2,2-trifluoroacetic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~100 mg/mL (~41.21 mM)
H2O : ~100 mg/mL (~41.21 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.4121 mL | 2.0604 mL | 4.1207 mL | |
| 5 mM | 0.0824 mL | 0.4121 mL | 0.8241 mL | |
| 10 mM | 0.0412 mL | 0.2060 mL | 0.4121 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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