TCRS-417
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.
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- 純度: 99.13%
- CAS 番号: 2032123-28-5
- 分子式: C25H19FN2O5
- 分子量:446.43
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 TCRS-417
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生物活性
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.
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.
化学情報
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CAS 番号 2032123-28-5
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性状 Solid
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分子量 446.43
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分子式 C25H19FN2O5
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Color Light yellow to brown
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SMILES
O=C(C1=CC(F)=CC=C1)NC2=CC=C(C3=C2C=CC=C3)OCC(NC4=CC=C(C(O)=C4)O)=O
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別名
T417
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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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Journal Impact Factor
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Most Recent
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Science
2025 Nov 6;390(6773):eads7152. PMID: 41197002
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (276 KB)
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SDS (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Small molecule compounds targeting pbx1 transcriptional complex.WO2016172437.
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
TCRS-417 関連分類
HY-153916 関連分類
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