TPCA-1
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MedKoo CAT#: 406590

CAS#: 507475-17-4

Description: TPCA-1 is a potent IKK-2 inhibitor. TPCA-1 is also an effective inhibitor of STAT3 phosphorylation, DNA binding, and transactivation in vivo. It selectively repressed proliferation of NSCLC cells with constitutive STAT3 activation. TPCA-1 as a direct dual inhibitor for both IKKs and STAT3, whereas treatment targeting EGFR only could not sufficiently repress NF-κB and STAT3 pathways for lung cancers harboring mutant EGFR. Therefore, synergistic treatment of TPCA-1 with TKIs has potential to be a more effective strategy for cancers.


Chemical Structure

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TPCA-1
CAS# 507475-17-4

Theoretical Analysis

MedKoo Cat#: 406590
Name: TPCA-1
CAS#: 507475-17-4
Chemical Formula: C12H10FN3O2S
Exact Mass: 279.0478
Molecular Weight: 279.29
Elemental Analysis: C, 51.61; H, 3.61; F, 6.80; N, 15.05; O, 11.46; S, 11.48

Price and Availability

Size Price Availability Quantity
25.0mg USD 150.0 2 Weeks
50.0mg USD 250.0 2 Weeks
100.0mg USD 450.0 2 Weeks
200.0mg USD 850.0 2 Weeks
500.0mg USD 1950.0 2 Weeks
1.0g USD 2950.0 2 Weeks
2.0g USD 5650.0 2 Weeks
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Synonym: TPCA1; TPCA 1; TPCA1

IUPAC/Chemical Name: 5-(4-fluorophenyl)-2-ureidothiophene-3-carboxamide

InChi Key: SAYGKHKXGCPTLX-UHFFFAOYSA-N

InChi Code: InChI=1S/C12H10FN3O2S/c13-7-3-1-6(2-4-7)9-5-8(10(14)17)11(19-9)16-12(15)18/h1-5H,(H2,14,17)(H3,15,16,18)

SMILES Code: O=C(C1=C(NC(N)=O)SC(C2=CC=C(F)C=C2)=C1)N

Appearance: Solid powder

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: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

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

Preparing Stock Solutions

The following data is based on the product molecular weight 279.29 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.

Recalculate based on batch purity %
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

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1: Nan J, Du Y, Chen X, Bai Q, Wang Y, Zhang X, Zhu N, Zhang J, Hou J, Wang Q, Yang J. TPCA-1 is a direct dual inhibitor of STAT3 and NF-κB and regresses mutant EGFR-associated human non-small cell lung cancers. Mol Cancer Ther. 2014 Mar;13(3):617-29. doi: 10.1158/1535-7163.MCT-13-0464. Epub 2014 Jan 8. PubMed PMID: 24401319.

2: Du Z, Whitt MA, Baumann J, Garner JM, Morton CL, Davidoff AM, Pfeffer LM. Inhibition of type I interferon-mediated antiviral action in human glioma cells by the IKK inhibitors BMS-345541 and TPCA-1. J Interferon Cytokine Res. 2012 Aug;32(8):368-77. doi: 10.1089/jir.2012.0002. Epub 2012 Apr 17. PubMed PMID: 22509977; PubMed Central PMCID: PMC3422054.

3: Sachse F, Becker K, Basel TJ, Weiss D, Rudack C. IKK-2 inhibitor TPCA-1 represses nasal epithelial inflammation in vitro. Rhinology. 2011 Jun;49(2):168-73. doi: 10.4193/Rhino10.099. PubMed PMID: 21743871.

4: Podolin PL, Callahan JF, Bolognese BJ, Li YH, Carlson K, Davis TG, Mellor GW, Evans C, Roshak AK. Attenuation of murine collagen-induced arthritis by a novel, potent, selective small molecule inhibitor of IkappaB Kinase 2, TPCA-1 (2-[(aminocarbonyl)amino]-5-(4-fluorophenyl)-3-thiophenecarboxamide), occurs via reduction of proinflammatory cytokines and antigen-induced T cell Proliferation. J Pharmacol Exp Ther. 2005 Jan;312(1):373-81. Epub 2004 Aug 17. PubMed PMID: 15316093.

TPCA-1

25.0mg / USD 150.0


Additional Information