| Field | Specification |
|---|---|
| Alternative names | T417 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C25H19FN2O5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
TCRS-417, also known as T417, is a small-molecule inhibitor of PBX1 that can directly block PBX1 binding to DNA (IC50 = 6.58 μM) and affects PBX1 transcription. By targeting the PBX1 signaling cascade, it reverses the stemness traits of Carboplatin-resistant (CR) cells toward a differentiated state, and it significantly suppresses the self-renewal and proliferation of cancer cells expressing high levels of PBX1. It can also decrease mRNA levels of FOXM1, NEK2, and E2F2 in cancer cell lines and is selectively toxic to chr1q-amp myeloma and solid tumor cells[1][2][3][4]. It is supplied as a solid (C25H19FN2O5, MW 446.43) at 99.13% purity.
Physical & Chemical Properties
| CAS Number | 2032123-28-5 |
|---|---|
| Molecular Formula | C25H19FN2O5 |
| Molecular Weight | 446.43 g/mol |
| Purity | 99.13% |
| Appearance | Solid |
| SMILES | O=C(C1=CC(F)=CC=C1)NC2=CC=C(C3=C2C=CC=C3)OCC(NC4=CC=C(C(O)=C4)O)=O |
| Signaling Pathway | Cell Cycle/DNA Damage |
| Solubility | In Vitro: DMSO: 100 mg/mL (224.00 mM; Requires sonication and warming and heat to 60°C; 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.
[1]. Small molecule compounds targeting pbx1 transcriptional complex.WO2016172437.
[2]. Yao-An Shen, et al., Abstract 1966: A novel small-molecule compound targeting PBX1-DNA interaction impedes cancer cell survival and carboplatin resistance. Cancer Res 1 July 2018; 78 (13_Supplement): 1966.
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 (224.00 mM) | requires sonication and warming and heat to 60°C; 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.
Data provided by the manufacturer.
In Vitro
TCRS-417 (20 μM, 48 h) produces significant depletion of the G2/M phase along with G0/1 phase arrest in 1 brain cancer (SNB-75), 2 lung cancer (A549, H69AR), 2 ovarian cancer (OVCAR3, A2780), 2 breast cancer (MCF-7, LTED), and 4 myeloma (MM.1S, U266, NCU.MM1, OPM2) cell lines after T417 treatment[3]. TCRS-417 (20 μM, 16-20 h) significantly lowers FOXM1, NEK2, and E2F2 mRNA levels in nearly all 11 cell lines[3]. TCRS-417 (0.625-80 μM) reduces PBX1 binding to DNA in a dose-dependent manner[4]. In OVCAR3-CR and SKOV3-CR cell lines, TCRS-417 (0-10 μM) weakens spherogenic capacity and shifts stem cell-like cells back toward a more differentiated state[4].
In Vivo
In a xenograft myeloma mouse model, TCRS-417 (10 mg/kg, s.c., 23 d) significantly decreases tumor size and weight[3]. TCRS-417 (5 mg/kg/injection, intratumoral, 3 doses weekly over a course of 3 weeks) lowers MEOX1 and BCL6 gene expression in a dose-dependent manner[4]. When combined with Carboplatin, TCRS-417 (5 mg/kg/injection, s.c., 3 doses weekly over a course of 3 weeks) significantly delays tumor growth and lowers the end point tumor weight of A2780 xenografts in immunocompromised nu/nu mice[4].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
Need this compound in a format that drops straight into your assay? We can tailor formulation, chemistry, and documentation so your results stay consistent across runs and re-orders.
- Format options: solid or pre-dissolved solution (choose solvent), target concentration, aliquots, light/moisture-protected packaging
- Chemistry options: free base/acid vs salt forms, hydrate/solvate preference, stereoisomer control (single enantiomer or racemate), close analogs
- Add-on labels & handles: D/¹³C/¹⁵N isotopes (LC-MS/internal standards), azide/alkyne or other functional handles for conjugation
- QC & documentation: standard COA or enhanced analytical pack (HPLC/LC-MS/NMR), chiral purity, residual solvents, water content (KF), method-specific specs
- Scale & continuity: mg to gram scale, bulk pricing, lot reservation, repeat-order continuity
To quote quickly, tell us: compound name + CAS/structure (SMILES or mol file), intended assay context, solvent preference, salt/stereochemistry requirements, purity/QC level, and the amount (mg–g).
Can’t find the compound you’re looking for?
Send the CAS or structure and your specs. We can help source it, suggest close equivalents, or discuss custom synthesis with the right QC documentation (RUO).
Direct targeting and regulation of RNA polymerase II by cell signaling kinases. Science 2025 Nov 6;390(6773):eads7152. PMID: 41197002
