Synonym
TD52; TD-52; TD 52; erlotinib derivative; erlotinib analogue;
IUPAC/Chemical Name
N2,N3-bis(3-ethynylphenyl)quinoxaline-2,3-diamine
InChi Key
SCUPZFSEJFWQIS-UHFFFAOYSA-N
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)
SMILES Code
C#CC1=CC=CC(NC2=NC3=CC=CC=C3N=C2NC4=CC=CC(C#C)=C4)=C1
Appearance
To be determined
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Protein phosphatase 2A (PP2A) is a tumor suppressor, which is functionally defective in various cancers. Previously, we found that PP2A activity determined the anticancer effect of bortezomib and erlotinib in hepatocellular carcinoma (HCC) cell
Preparing Stock Solutions
The following data is based on the
product
molecular weight
360.42
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Liu CY, Huang TT, Huang CT, Hu MH, Wang DS, Wang WL, Tsai WC, Lee CH, Lau KY, Yang HP, Chen MH, Shiau CW, Tseng LM, Chen KF. 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. doi: 10.1016/j.ejca.2016.11.012. Epub 2016 Dec 24. PMID: 28027514.
2: Yu HC, Hung MH, Chen YL, Chu PY, Wang CY, Chao TT, Liu CY, Shiau CW, Chen KF. Erlotinib derivative inhibits hepatocellular carcinoma by targeting CIP2A to reactivate protein phosphatase 2A. Cell Death Dis. 2014 Jul 31;5(7):e1359. doi: 10.1038/cddis.2014.325. PMID: 25077545; PMCID: PMC4123111.
3: Crugliano T, Quaresima B, Gaspari M, Faniello MC, Romeo F, Baudi F, Cuda G, Costanzo F, Venuta S. Specific changes in the proteomic pattern produced by the BRCA1-Ser1841Asn missense mutation. Int J Biochem Cell Biol. 2007;39(1):220-6. doi: 10.1016/j.biocel.2006.08.005. Epub 2006 Aug 30. Erratum in: Int J Biochem Cell Biol. 2017 Jul;88:236-237. PMID: 17005433.
