Cat. No.: HY-135699

TD52

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Based on 2 publication(s) in Google Scholar

TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity. TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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Pureté: 95.0%
CAS No.: 1798328-24-1
Formule: C₂₄H₁₆N₄
Masse moléculaire:360.41

Stockage:

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

TD52 Chemical Structure

CAS No.: 1798328-24-1

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Activité biologique
- Description
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

TD52, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 has less p-EGFR inhibition and has potent anti-cancer activity^[1]. TD52 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

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In Vitro

TD52 (2-10 μM; 48 hours) shows anti-proliferative ability and induces differential apoptotic effects in these cell lines^[1].
TD52 (5 μM; 48 hours) has minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression^[1].
TD52 (2.5, 5, 7.5 μM; 48 hours) time-dependently induces apoptosis accompanied with downregulating CIP2A and p-Akt^[1].
TD52 (5 μM; 24 hours) significantly increases the phosphatase activity of PP2A in TNBC cells^[1].
TD52 (5 μM; 48 hours) has no obvious effects on other common RTKs, such as IGFR, PDGFR and VEGFR2^[1].

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

Apoptosis Analysis^[1]

Cell Line:

Three TNBC cell lines including HCC-1937, MDA-MB-231 and MDA-MB-468 cells
Concentration:

2, 4, 6, 8, 10 μM
Incubation Time:

48 hours
Result:

Showed anti-proliferative ability and induced differential apoptotic effects in these cell lines.

Western Blot Analysis^[1]

Cell Line:

MDA-MB-231 cell
Concentration:

5 μM
Incubation Time:

48 hours
Result:

Had minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression.

In Vivo

TD52 (10 mg/kg/day; oral gavage; for 52 days) significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight^[1].

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

Animal Model:

Female NCr athymic nude mice (5-7 weeks of age)^[1]
Dosage:

10 mg/kg
Administration:

Oral gavage; daily; for 52 days
Result:

Significantly inhibits MDA-MB-468 xenograft tumour size and tumour weight.
Decreased the protein expressions of CIP2A and p-Akt in the three MDA-MB-468 xenograft tumours.

Chemical Information

CAS No. 1798328-24-1
Appearance Solid
Masse moléculaire 360.41
Formule C₂₄H₁₆N₄
Color White to yellow
SMILES

C#CC1=CC(NC2=NC3=CC=CC=C3N=C2NC4=CC=CC(C#C)=C4)=CC=C1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Cell Mol Biol Lett

CIP2A promotes inflammation and exacerbates osteoarthritis by targeting CEMIP. [Abstract]

2025 Jun 9;30(1):67. PMID: 40490703
Mol Cell Endocrinol

cAMP/PKA signaling promotes AKT deactivation by reducing CIP2A expression, thereby facilitating decidualization. [Abstract]

2023 Jul 1:571:111946. PMID: 37127088

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (277.46 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7746 mL

13.8731 mL

27.7462 mL

5 mM

0.5549 mL

2.7746 mL

5.5492 mL

10 mM

0.2775 mL

1.3873 mL

2.7746 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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 (6.94 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.94 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

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.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (280 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 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)
Instruction de manipulation (2659 KB)

Références

[1]. Chun-Yu Liu, et al. EGFR-independent Elk1/CIP2A signalling mediates apoptotic effect of an erlotinib derivative TD52 in triple-negative breast cancer cells. Eur J Cancer. 2017 Feb;72:112-123. [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	2.7746 mL	13.8731 mL	27.7462 mL	69.3654 mL
	5 mM	0.5549 mL	2.7746 mL	5.5492 mL	13.8731 mL
	10 mM	0.2775 mL	1.3873 mL	2.7746 mL	6.9365 mL
	15 mM	0.1850 mL	0.9249 mL	1.8497 mL	4.6244 mL
	20 mM	0.1387 mL	0.6937 mL	1.3873 mL	3.4683 mL
	25 mM	0.1110 mL	0.5549 mL	1.1098 mL	2.7746 mL
	30 mM	0.0925 mL	0.4624 mL	0.9249 mL	2.3122 mL
	40 mM	0.0694 mL	0.3468 mL	0.6937 mL	1.7341 mL
	50 mM	0.0555 mL	0.2775 mL	0.5549 mL	1.3873 mL
	60 mM	0.0462 mL	0.2312 mL	0.4624 mL	1.1561 mL
	80 mM	0.0347 mL	0.1734 mL	0.3468 mL	0.8671 mL
	100 mM	0.0277 mL	0.1387 mL	0.2775 mL	0.6937 mL

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TD52

Apoptosis Compound Library

Kinase Inhibitor Library

Metabolism/Protease Compound Library

PI3K/Akt/mTOR Compound Library

Stem Cell Signaling Compound Library

Anti-Cancer Compound Library

Autophagy Compound Library

Anti-Aging Compound Library

Differentiation Inducing Compound Library

Oxygen Sensing Compound Library

Glycolysis Compound Library

Cytoskeleton Compound Library

Orally Active Compound Library

Glutamine Metabolism Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Cancer Metabolism Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Glucose Metabolism Compound Library

Targeted Diversity Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Cancer Stem Cells Compound Library

Pain-Related Compound Library

Metabolic Enzyme Compound Library

Cell Death Library

Serine/Threonine Kinase Inhibitor Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Lactylation Compound Library

Alkyne Compound Library

Publications Citing Use of MedChemExpress (MCE) TD52

Voir tous les produits spécifiques à Isoform Akt

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

TD52 Related Classifications

HY-135699 Related Classifications