Cat. No.: HY-153916

TCRS-417

(Synonyms: T417)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

TCRS-417 (T417) is a small-molecular inhibitor for PBX1. TCRS-417 can directly block PBX1-binding to DNA (IC₅₀ = 6.58 μM), and affects PBX1 transcription. TCRS-417 is able to hammer out the stemness traits of Carboplatin (HY-17393)-resistant (CR) cells to revert to a differentiated status through tacking PBX1 signaling cascade. TCRS-417 significantly suppresses self-renewal and proliferation of cancer cells expressing high levels of PBX1. TCRS-417 can decrease the mRNA levels of FOXM1, NEK2, and E2F2 in cancer cell lines. TCRS-417 is selectively toxic against chr1q-amp myeloma and solid tumor cells.

For research use only. We do not sell to patients.

Purity: 99.13%
CAS No.: 2032123-28-5
Formula: C₂₅H₁₉FN₂O₅
Molecular Weight:446.43

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

TCRS-417 Chemical Structure

CAS No.: 2032123-28-5

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

All DNA/RNA Synthesis Isoforms :

All NEKs Isoforms :

In Vitro

TCRS-417 (Compound T417) (20 μM, 48 h) results in significant depletion of the G2/M phase, together with G0/1 phase arrest, upon T417 treatment in 4 myeloma (MM.1S, U266, NCU.MM1, OPM2), 2 breast cancer (MCF-7, LTED), 2 ovarian cancer (OVCAR3, A2780), 2 lung cancer (A549, H69AR), and 1 brain cancer (SNB-75) cell lines^[3].
TCRS-417 (20 μM, 16-20 h) significantly decreases the mRNA levels of FOXM1, NEK2, and E2F2 in almost all 11 cell lines^[3].
TCRS-417 (0.625-80 μM) decreases the PBX1 binding to the DNA in a dose-dependent manner^[4].
TCRS-417 (0-10 μM) attenuates the spherogenic capacity and re-directs stem cell-like cells back to a more differentiated state in OVCAR3-CR and SKOV3-CR cell lines^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

TCRS-417 (Compound T417) (10 mg/kg, s.c., 23 d) significantly reduces tumor size and weight in xenograft myeloma mice model^[3].
TCRS-417 (5 mg/kg/injection, intratumoral, 3 doses per week over a course of 3 weeks) reduces MEOX1 and BCL6 gene expression in a dose-dependent manner^[4].
TCRS-417 (5 mg/kg/injection, s.c., 3 doses per week over a course of 3 weeks) significantly delays tumor growth and reduced the end point tumor weight of A2780 xenografts when combined with Carboplatin (HY-17393) in immunocompromised nu/nu mice^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 2032123-28-5
Appearance Solid
Molecular Weight 446.43
Formula C₂₅H₁₉FN₂O₅
Color Light yellow to brown
SMILES

O=C(C1=CC(F)=CC=C1)NC2=CC=C(C3=C2C=CC=C3)OCC(NC4=CC=C(C(O)=C4)O)=O
Synonyms

T417
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (1)

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Science

Direct targeting and regulation of RNA polymerase II by cell signaling kinases. [Abstract]

2025 Nov 6;390(6773):eads7152. PMID: 41197002

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (224.00 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2400 mL

11.2000 mL

22.3999 mL

5 mM

0.4480 mL

2.2400 mL

4.4800 mL

10 mM

0.2240 mL

1.1200 mL

2.2400 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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.

[3]. Trasanidis, N., et al., (2022). Systems medicine dissection of chr1q-amp reveals a novel PBX1-FOXM1 axis for targeted therapy in multiple myeloma. Blood, 139(13), 1939–1953. [Content Brief]

[4]. Shen, Y. A., et al., (2021). Development of small molecule inhibitors targeting PBX1 transcription signaling as a novel cancer therapeutic strategy. iScience, 24(11), 103297. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2400 mL	11.2000 mL	22.3999 mL	55.9998 mL
	5 mM	0.4480 mL	2.2400 mL	4.4800 mL	11.2000 mL
	10 mM	0.2240 mL	1.1200 mL	2.2400 mL	5.6000 mL
	15 mM	0.1493 mL	0.7467 mL	1.4933 mL	3.7333 mL
	20 mM	0.1120 mL	0.5600 mL	1.1200 mL	2.8000 mL
	25 mM	0.0896 mL	0.4480 mL	0.8960 mL	2.2400 mL
	30 mM	0.0747 mL	0.3733 mL	0.7467 mL	1.8667 mL
	40 mM	0.0560 mL	0.2800 mL	0.5600 mL	1.4000 mL
	50 mM	0.0448 mL	0.2240 mL	0.4480 mL	1.1200 mL
	60 mM	0.0373 mL	0.1867 mL	0.3733 mL	0.9333 mL
	80 mM	0.0280 mL	0.1400 mL	0.2800 mL	0.7000 mL
	100 mM	0.0224 mL	0.1120 mL	0.2240 mL	0.5600 mL

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TCRS-417

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Extracellular Vesicles (EVs) Compound Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) TCRS-417

All DNA/RNA Synthesis Isoforms

All NEKs Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

TCRS-417

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Extracellular Vesicles (EVs) Compound Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Bioactive Compound Library Max

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) TCRS-417

All DNA/RNA Synthesis Isoforms

All NEKs Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

TCRS-417 Related Classifications

Cat. No.: HY-153916