TP-472
Based on 2 publication(s) in Google Scholar
TP-472, a chemical probe, is a selective BRD9/7 inhibitor, with Kds of 33 nM and 340 nM for BRD9 and BRD7, respectively. TP-472 exhibits >30-fold selectivity for BRD9 over other bromodomain family members except BRD7. TP-472 induces apoptosis of melanoma cells.
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- Pureza: 99.54%
- No. CAS: 2079895-62-6
- Fòrmula: C20H19N3O2
- Peso molecular:333.38
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) TP-472
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Actividad biológica
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BRD9 33 nM (Kd) |
BRD7 0.34 μM (Kd) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | GI50 |
1.33 μM
Compound: 16; TP 472
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Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
Growth inhibition of human HL60 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
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[PMID: 33275431] |
| MCF7 | GI50 |
4.49 μM
Compound: 16; TP 472
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Growth inhibition of human MCF7 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
Growth inhibition of human MCF7 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
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[PMID: 33275431] |
| MDA-MB-231 | IC50 |
12 μM
Compound: 1; TP-472
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Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTS assay
Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTS assay
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[PMID: 27935314] |
| SK-MEL-5 | GI50 |
2.77 μM
Compound: 16; TP 472
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Growth inhibition of human SK-MEL-5 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
Growth inhibition of human SK-MEL-5 cells after 72 hrs by CellTiter 96S AQeous non-radioactive cell proliferation assay
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[PMID: 33275431] |
TP-472 (1 μM, 3 μM; 24-216 hours) yields concentration-dependent growth defects in ESCs[2].
TP-472 (0.1-10 μM; 24 h) effectively inhibits the growth of both the BRAF mutant melanoma cell lines at 5 and 10 μM concentrations[3].
TP-472 (for 2 weeks) also strongly inhibits the long-term survival of multiple melanoma cell lines (M14, SKMEL-28, A375, and A2058) at concentrations of 5 and 10 μM[3].
TP-472 (5-10 μM; 24 h) treatment downregulates genes encoding various extracellular matrix (ECM) proteins, including integrins, collagens, and fibronectins in A375 cells[3].
TP-472 (0.1-10 μM; 24 h) results in the upregulation of pro-apoptotic genes (BAX, MDM2, CDKN1A) in A375 cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Embryonic stem cells
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Concentration:1 µM, 3 µM
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Incubation Time:24 hours, 72 hours, 120 hours, 168 hours, 216 hours
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Result:Yields concentration-dependent growth defects in ESCs.
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Cell Line:M14 and SKMEL-28 cells[3]
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Concentration:0.1 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 10 μM
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Incubation Time:24 h
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Result:Effectively inhibited the growth of both the BRAF mutant melanoma cell lines.
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Cell Line:A375 cells
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Concentration:10 μM
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Incubation Time:24 h
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Result:Resulted in the upregulation of pro-apoptotic genes.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NSG mice injected with A375-MA2 cells (male five- to six-week-old)[3]
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Dosage:20 mg/kg
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Administration:i.p.; three times a week; for 5 weeks
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Result:Significantly inhibited the subcutaneous tumor growth in melanoma xenograft mouse model.
Chemical Information
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No. CAS 2079895-62-6
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Appearance Solid
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Peso molecular 333.38
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Fòrmula C20H19N3O2
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Color Light yellow to yellow
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SMILES
O=C(C)C1=CC(C2=C(C)C=CC(C(NC3CC3)=O)=C2)=C4N=CC=CN41
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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bioRxiv
Radiation synergizes with BET inhibition to stimulate durable, systemic anti-tumor immunity in murine cancer models. [Abstract]2026 Feb 18:2026.02.16.706212. PMID: 41757027 -
Solvente y solubilidad
DMSO : 100 mg/mL (299.96 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.50 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (283 KB)
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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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Moustakim M, et al. Chemical probes and inhibitors of bromodomains outside the BET family. Medchemcomm. 2016 Dec 7;7(12):2246-2264. [Content Brief]
[2]. Gatchalian J, et al. A non-canonical BRD9-containing BAF chromatin remodeling complex regulates naive pluripotency in mouse embryonic stem cells. Nat Commun. 2018 Dec 3;9(1):5139. [Content Brief]
[3]. Lawrence David Mason, et al. The BRD9/7 Inhibitor TP-472 Blocks Melanoma Tumor Growth by Suppressing ECM-Mediated Oncogenic Signaling and Inducing Apoptosis. Cancers (Basel). 2021 Nov 3;13(21):5516. [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 | 2.9996 mL | 14.9979 mL | 29.9958 mL | 74.9895 mL |
| 5 mM | 0.5999 mL | 2.9996 mL | 5.9992 mL | 14.9979 mL | |
| 10 mM | 0.3000 mL | 1.4998 mL | 2.9996 mL | 7.4990 mL | |
| 15 mM | 0.2000 mL | 0.9999 mL | 1.9997 mL | 4.9993 mL | |
| 20 mM | 0.1500 mL | 0.7499 mL | 1.4998 mL | 3.7495 mL | |
| 25 mM | 0.1200 mL | 0.5999 mL | 1.1998 mL | 2.9996 mL | |
| 30 mM | 0.1000 mL | 0.4999 mL | 0.9999 mL | 2.4997 mL | |
| 40 mM | 0.0750 mL | 0.3749 mL | 0.7499 mL | 1.8747 mL | |
| 50 mM | 0.0600 mL | 0.3000 mL | 0.5999 mL | 1.4998 mL | |
| 60 mM | 0.0500 mL | 0.2500 mL | 0.4999 mL | 1.2498 mL | |
| 80 mM | 0.0375 mL | 0.1875 mL | 0.3749 mL | 0.9374 mL | |
| 100 mM | 0.0300 mL | 0.1500 mL | 0.3000 mL | 0.7499 mL |
TP-472 Related Classifications
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