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

TD52 

Cat. No.: HY-135699 Purity: ≥95.0%
Handling Instructions

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.

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

TD52 Chemical Structure

TD52 Chemical Structure

CAS No. : 1798328-24-1

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 132 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 210 In-stock
Estimated Time of Arrival: December 31
25 mg USD 420 In-stock
Estimated Time of Arrival: December 31
50 mg USD 720 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1250 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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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].

IC50 & Target[1]

Akt

 

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].

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].

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.
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)

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
10 mM 0.2775 mL 1.3873 mL 2.7746 mL
*Please refer to the solubility information to select the appropriate solvent.
References
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TD52
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