2. Apoptosis Metabolic Enzyme/Protease PI3K/Akt/mTOR
  3. Apoptosis Phosphatase Akt
  4. TD52

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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TD52 Chemical Structure

TD52 Chemical Structure

CAS No. : 1798328-24-1

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Based on 1 publication(s) in Google Scholar

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TD52 Related Antibodies

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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.

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.

TD52 Related Antibodies

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.
Molecular Weight

360.41

Formula

C24H16N4
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

C#CC1=CC(NC2=NC3=CC=CC=C3N=C2NC4=CC=CC(C#C)=C4)=CC=C1
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 (277.46 mM; Need ultrasonic; 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 2.7746 mL 13.8731 mL 27.7462 mL
5 mM 0.5549 mL 2.7746 mL 5.5492 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)

Mass
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Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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 (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.

    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 (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.

    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)

g

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: ≥95.0%

SDS (251 KB)

COA (252 KB) HNMR (255 KB)

Handling Instructions (2659 KB)
References

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 2.7746 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 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:

TD521798328-24-1TD 52TD-52ApoptosisPhosphataseAktPKBProtein kinase BErlotiniborallyCIP2Atriple-negativebreastcancerTNBCPP2Ap-AktElk1p-EGFRHCC-1937MDA-MB-231MDA-MB-468Inhibitorinhibitorinhibit

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