A derivative of erlotinib

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TD52

Name: TD52
Brand: -

Item No. 37744

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)

Technical Information

Formal Name

N²,N³-bis(3-ethynylphenyl)-2,3-quinoxalinediamine

CAS Number

1798328-24-1

Molecular Formula

C₂₄H₁₆N₄

Formula Weight

360.4

Purity

≥98%

Formulation (Request formulation change)

A solid

Solubility(Learn about Variance in Solubility)

DMF: 5 mg/mlDMSO: 5 mg/ml

λ_max

237, 246, 277, 366 nm

SMILES

C#CC1=CC=CC(NC2=NC3=C(N=C2NC4=CC(C#C)=CC=C4)C=CC=C3)=C1

InChi Code

InChI=1S/C24H16N4/c1-3-17-9-7-11-19(15-17)25-23-24(26-20-12-8-10-18(4-2)16-20)28-22-14-6-5-13-21(22)27-23/h1-2,5-16H,(H,25,27)(H,26,28)

InChi Key

SCUPZFSEJFWQIS-UHFFFAOYSA-N

Shipping & Storage Information

Storage

-20°C

Shipping

Room temperature in continental US; may vary elsewhere

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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5 mg

$95

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10 mg

$180

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25 mg

$354

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50 mg

$517

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Product Description

TD52 is a derivative of the EGFR tyrosine kinase inhibitor erlotinib (Item Nos. 10483 | 35517).¹ It decreases the viability of HA22T, Hep3B, PLC/PRF/5, and SK-HEP-1 hepatocellular carcinoma cells (IC₅₀s = 0.9, 0.9, 0.8, and 1.2 µM, respectively). TD52 induces apoptosis in a variety of cancer cells, including HA22T and Hep3B hepatocellular carcinoma and HCC1937 and MDA-MB-231 triple-negative breast cancer cells in a concentration-dependent manner.^1,2 TD52 (10 mg/kg per day) increases intratumoral protein phosphatase 2A (PP2A) activity, reduces intratumoral cancerous inhibitor of PP2A (CIP2A) and phosphorylated Akt levels, and reduces tumor growth in a PLC/PRF/5 mouse xenograft model.¹

WARNING This product is not for human or veterinary use.

References & Product Citations

Product Description References

1. Yu, H.-C., Hung, M.-H., Chen, Y.-L., et al. Erlotinib derivative inhibits hepatocellular carcinoma by targeting CIP2A to reactivate protein phosphatase 2A. Cell Death Dis. 5(7), e1359 (2014).

2. Liu, C.-Y., Huang, T.-T., Huang, C.-T., et al. EGFR-independent Elk1/CIP2A signalling mediates apoptotic effect of an erlotinib derivative TD52 in triple-negative breast cancer cells. Eur. J. Cancer 72, 112-123 (2017).

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