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

TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity. TD52 (dihydrochloride) 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 dihydrochloride Chemical Structure

TD52 dihydrochloride Chemical Structure

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 95 In-stock
Solid
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10 mg USD 160 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of TD52 dihydrochloride:

TD52 dihydrochloride Related Antibodies

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Description

TD52 dihydrochloride, an Erlotinib (HY-50896) derivative, is an orally active, potent cancerous inhibitor of protein phosphatase 2A (CIP2A) inhibitor. TD52 dihydrochloride mediates the apoptotic effect in triple-negative breast cancer (TNBC) cells via regulating the CIP2A/PP2A/p-Akt signalling pathway. TD52 dihydrochloride indirectly reduced CIP2A by disturbing Elk1 binding to the CIP2A promoter. TD52 dihydrochloride has less p-EGFR inhibition and has potent anti-cancer activity[1]. TD52 (dihydrochloride) 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 dihydrochloride (2-10 μM; 48 hours) shows anti-proliferative ability and induces differential apoptotic effects in these cell lines[1].
TD52 dihydrochloride (5 μM; 48 hours) has minimal effects on p-EGFR or EGFR expression but downregulated CIP2A expression[1].
TD52 dihydrochloride (2.5, 5, 7.5 μM; 48 hours) time-dependently induces apoptosis accompanied with downregulating CIP2A and p-Akt[1].
TD52 dihydrochloride (5 μM; 24 hours) significantly increases the phosphatase activity of PP2A in TNBC cells[1].
TD52 dihydrochloride (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 dihydrochloride Related Antibodies
In Vivo

TD52 dihydrochloride (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.
Molecular Weight

433.33

Formula

C24H18Cl2N4
Appearance

Solid

Color

Light yellow to yellow

SMILES

C#CC1=CC(NC2=NC3=CC=CC=C3N=C2NC4=CC=CC(C#C)=C4)=CC=C1.[H]Cl.[H]Cl
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 : 25 mg/mL (57.69 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 2.3077 mL 11.5386 mL 23.0771 mL
5 mM 0.4615 mL 2.3077 mL 4.6154 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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 2.3077 mL 11.5386 mL 23.0771 mL 57.6928 mL
5 mM 0.4615 mL 2.3077 mL 4.6154 mL 11.5386 mL
10 mM 0.2308 mL 1.1539 mL 2.3077 mL 5.7693 mL
15 mM 0.1538 mL 0.7692 mL 1.5385 mL 3.8462 mL
20 mM 0.1154 mL 0.5769 mL 1.1539 mL 2.8846 mL
25 mM 0.0923 mL 0.4615 mL 0.9231 mL 2.3077 mL
30 mM 0.0769 mL 0.3846 mL 0.7692 mL 1.9231 mL
40 mM 0.0577 mL 0.2885 mL 0.5769 mL 1.4423 mL
50 mM 0.0462 mL 0.2308 mL 0.4615 mL 1.1539 mL
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TD52 dihydrochloride 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:

TD52TD 52TD-52AktPhosphataseApoptosisPKBProtein kinase BErlotiniborallyCIP2Atriple-negativebreastcancerTNBCPP2Ap-AktElk1p-EGFRHCC-1937MDA-MB-231MDA-MB-468Inhibitorinhibitorinhibit

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