TP-472

Name: TP-472
Brand: MedChemExpress
SKU: HY-100517
Rating: 5.0 (1 reviews)

Cat. No.: HY-100517 Purity: 99.27%: FAQs
Data Sheet SDS COA Handling Instructions

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TP-472 is a selective BRD9/7 inhibitor, with K_ds 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.

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

TP-472 Chemical Structure

CAS No. : 2079895-62-6

Size	Price	Stock	Quantity
1 mg	USD 40	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 120	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 420	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 670	In-stock	Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

IC₅₀ & Target^[1]

BRD9

33 nM (Kd)

BRD7

0.34 μM (Kd)

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	GI₅₀	1.33 μM Compound: 16; TP 472	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	[PMID: 33275431]
MCF7	GI₅₀	4.49 μM Compound: 16; TP 472	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	[PMID: 33275431]
MDA-MB-231	IC₅₀	12 μM Compound: 1; TP-472	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	[PMID: 27935314]
SK-MEL-5	GI₅₀	2.77 μM Compound: 16; TP 472	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	[PMID: 33275431]

In Vitro

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.

Cell Viability Assay^[2]

Cell Line:	Embryonic stem cells
Concentration:	1 µM, 3 µM
Incubation Time:	24 hours, 72 hours, 120 hours, 168 hours, 216 hours
Result:	Yields concentration-dependent growth defects in ESCs.

Cell Proliferation Assay^[3]

Cell Line:	M14 and SKMEL-28 cells^[3]
Concentration:	0.1 μM, 0.5 μM, 1 μM, 2 μM, 5 μM, 10 μM
Incubation Time:	24 h
Result:	Effectively inhibited the growth of both the BRAF mutant melanoma cell lines.

Western Blot Analysis^[3]

Cell Line:	A375 cells
Concentration:	10 μM
Incubation Time:	24 h
Result:	Resulted in the upregulation of pro-apoptotic genes.

In Vivo

TP-472 (20 mg/kg; i.p.; three times a week; for 5 weeks) significantly inhibits the subcutaneous tumor growth in melanoma xenograft mouse model^[3].

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

Animal Model:	NSG mice injected with A375-MA2 cells (male five- to six-week-old)^[3]
Dosage:	20 mg/kg
Administration:	i.p.; three times a week; for 5 weeks
Result:	Significantly inhibited the subcutaneous tumor growth in melanoma xenograft mouse model.

Molecular Weight

333.38

Formula

C₂₀H₁₉N₃O₂

CAS No.

2079895-62-6

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C)C1=CC(C2=C(C)C=CC(C(NC3CC3)=O)=C2)=C4N=CC=CN41

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

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.9996 mL	14.9979 mL	29.9958 mL
5 mM	0.5999 mL	2.9996 mL	5.9992 mL
10 mM	0.3000 mL	1.4998 mL	2.9996 mL

View the 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.52%

Select Batch:

Data Sheet (282 KB) SDS (251 KB)

COA (256 KB) HNMR (157 KB) RP-HPLC (140 KB) LCMS (276 KB)

Handling Instructions (2659 KB)

References

[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

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

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TP-4722079895-62-6TP472TP 472Epigenetic Reader DomainApoptosisBRD9BRD9-BDBRD7bromodomainInhibitorinhibitorinhibit

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Complete Stock Solution Preparation Table

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