Antitumor agent-153

Name: Antitumor agent-153
Brand: MedChemExpress
SKU: HY-163518
Rating: 4.5 (1 reviews)

Cat. No.: HY-163518 Purity: 99.62%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

Antitumor agent-153 (compound 11b) is an optimized H2A histone ubiquitination inhibitor based on PRT4165 (HY-19817). Antitumor agent-153 inhibits the viability of human osteosarcoma U2OS cells and reduces histone H2A monoubiquitination, exhibiting anticancer activity.

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

Antitumor agent-153 Chemical Structure

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	Get quote
200 mg	Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

Cellular Effect

Cell Line	Type	Value	Description	References
U2OS	IC₅₀	5.86 μM Compound: 11b	Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs	[PMID: 38636717]

In Vitro

Antitumor agent-153 has an IC₅₀ of 5.86 μM on U2O cells and completely inhibits their proliferation at 30 μM ^[1].
Reduced H2AK119ub1 levels disrupt tumor development and cancer cell growth. Antitumor agent-153 (24-96 μM; 1 h) can significantly reduce H2AK119ub1 levels in U2O cells in a dose-dependent manner^[1].

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

Cell Viability Assay^[1]

Cell Line:	U2O cells
Concentration:	6 μM, 12 μM, 24 μM, 48 μM, 96 μM
Incubation Time:	1 h
Result:	Significantly decreased H2AK119ub1 levels in cells in a dose-dependent manner (24-96 μM).

Molecular Weight

324.24

Formula

C₁₆H₈N₂O₆

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C(C/2=O)C=CC=C1)C2=C/C3=C([N+]([O-])=O)C=CC=C3[N+]([O-])=O

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 (308.41 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	3.0841 mL	15.4207 mL	30.8414 mL
5 mM	0.6168 mL	3.0841 mL	6.1683 mL
10 mM	0.3084 mL	1.5421 mL	3.0841 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: ≥ 5 mg/mL (15.42 mM); Suspended solution

This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.

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: 99.62%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (254 KB) HNMR (94 KB) RP-HPLC (194 KB) LCMS (90 KB)

Handling Instructions (2659 KB)

References

[1]. Ni S, et al. Identification of a novel histone H2A mono-ubiquitination-inhibiting cell-active small molecule. Bioorg Med Chem Lett. 2024 Jun 1;105:129759. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0841 mL	15.4207 mL	30.8414 mL	77.1034 mL
	5 mM	0.6168 mL	3.0841 mL	6.1683 mL	15.4207 mL
	10 mM	0.3084 mL	1.5421 mL	3.0841 mL	7.7103 mL
	15 mM	0.2056 mL	1.0280 mL	2.0561 mL	5.1402 mL
	20 mM	0.1542 mL	0.7710 mL	1.5421 mL	3.8552 mL
	25 mM	0.1234 mL	0.6168 mL	1.2337 mL	3.0841 mL
	30 mM	0.1028 mL	0.5140 mL	1.0280 mL	2.5701 mL
	40 mM	0.0771 mL	0.3855 mL	0.7710 mL	1.9276 mL
	50 mM	0.0617 mL	0.3084 mL	0.6168 mL	1.5421 mL
	60 mM	0.0514 mL	0.2570 mL	0.5140 mL	1.2851 mL
	80 mM	0.0386 mL	0.1928 mL	0.3855 mL	0.9638 mL
	100 mM	0.0308 mL	0.1542 mL	0.3084 mL	0.7710 mL