| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C25H29N5O2S |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
CT1113 is a selective, orally active inhibitor of USP25/USP28 that inhibits cancer cell proliferation, induces apoptosis, and causes G2/S phase cell cycle arrest. It reduces levels of total and phosphorylated BCR-ABL1 as well as total and phosphorylated STAT5, without altering BCR-ABL1 mRNA levels, and it is applicable to research on pancreatic cancer, colon cancer, and acute leukemia[1][2]. It is supplied as a light yellow to yellow solid (C25H29N5O2S, MW 463.60) at 99.61% purity.
Physical & Chemical Properties
| CAS Number | 2523435-18-7 |
|---|---|
| Molecular Formula | C25H29N5O2S |
| Molecular Weight | 463.60 g/mol |
| Purity | 99.61% |
| Appearance | Solid |
| Color | Light yellow to yellow |
| SMILES | CNC1=C(C(N[C@@H]2CC3=CC=C(N4CC5NC(CC5)C4)C=C3OC2)=O)SC6=NC(C)=CC=C16 |
| Target | STAT5, BCR-ABL1 |
| Signaling Pathway | Cell Cycle/DNA Damage; Apoptosis; Protein Tyrosine Kinase/RTK; JAK/STAT Signaling; Stem Cell/Wnt |
| Solubility | In Vitro: DMSO: 100 mg/mL (215.70 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 6 months; -20°C, 1 month. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
[2]. Shi T, et al. CT1113, a Potent, Oral Small Molecule Inhibitor of USP25, Demonstrates Anti-Tumor Activity in Ph-Positive Acute Lymphoblastic Leukaemia. Blood. 2024 Nov 5;144:4168.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 100 mg/mL (215.70 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 5 mg/mL (10.79 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 5 mg/mL (10.79 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 5 mg/mL (10.79 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 5 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
CT1113 (500 nM; 1-24 h) lowers c-MYC levels in various cancer cell lines within 1-2 h, reduces USP25, USP28, LSD1 and Tankyrase levels after 24 h, and increases ubiquitination of c-MYC and Tankyrase, with no effect on the stability of p53 or CHK2[1]. CT1113 potently blocks proliferation of various tumor cell lines, giving an EC50 of 65 nM in control HCT116 cells; the antiproliferative effect is largely targeted, because co-overexpression of USP25 and USP28 lowers the sensitivity of cells to CT1113[1]. In vitro, CT1113 (0-600 nM; 72 h) potently suppresses growth of primary Ph+ALL cells, Ba/F3 cells expressing mutant BCR-ABL1, and human Ph+ALL cell lines, with an IC50 of about 200 nM[2]. CT1113 (0-600 nM; 72 h) significantly triggers apoptosis in primary Ph+ALL cells, Ba/F3 cells expressing mutant BCR-ABL1, and human Ph+ALL cell lines[2]. In human Ph+ALL cell lines, CT1113 (0-600 nM; 72 h) blocks phosphorylation of BCR-ABL1 and STAT5 and lowers total BCR-ABL1 and STAT5 protein levels (proteasome inhibition can block this effect)[2]. CT1113 (0-600 nM; 72 h) raises the ubiquitination level of BCR-ABL1 in human Ph+ALL cell lines, thereby promoting its proteasomal degradation[2]. BCR-ABL1 mRNA levels in human Ph+ALL cell lines are not changed by CT1113 (0-600 nM; 72 h)[2].
Western Blot Analysis[1]
| Cell Line | HCT116, HGC27, SMMC7721, diverse cancer cell lines |
|---|---|
| Concentration | 500 nM |
| Incubation Time | 24 h |
| Result | Dramatically reduced c-MYC levels within 1-2 h across diverse cancer cell lines.\n Dramatically decreased levels of USP25, USP28, LSD1, and Tankyrase after 24 h of treatment with 500 nM.\n Increased ubiquitination of c-MYC and Tankyrase proteins.\nShowed no significant destabilization of p53 or CHK2 proteins. |
In Vivo
In a mouse pancreatic cancer xenograft model, CT1113 shows strong anti-tumor activity, with significant suppression of tumor growth, lower c-MYC levels, and reduced tumor cell proliferation[1]. In a mouse colon cancer CDX model, CT1113 displays strong anti-tumor activity and significantly suppresses tumor growth[1]. In healthy C57BL/6 mice, CT1113 (21 days) treatment leads to reversible mild body weight loss without overt toxicity; intestinal crypt proliferation is not disrupted despite lower overall intestinal c-MYC levels, and testicular tissue structure and spermatogonia proliferation are not impaired[1].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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