TC-S 7006
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 562293

CAS#: 871307-18-5

Description: TC-S 7006 is a selective Tpl2 (Cot; MAP3K8) inhibitor.

Chemical Structure

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TC-S 7006
CAS# 871307-18-5
Instruction

Theoretical Analysis

MedKoo Cat#: 562293
Name: TC-S 7006
CAS#: 871307-18-5
Chemical Formula: C21H14ClFN6
Exact Mass: 404.10
Molecular Weight: 404.830
Elemental Analysis: C, 62.30; H, 3.49; Cl, 8.76; F, 4.69; N, 20.76

Price and Availability

Size Price Availability Quantity
5mg USD 300 2 Weeks
10mg USD 500 2 Weeks
25mg USD 950 2 Weeks
Bulk inquiry

Synonym: TC-S 7006; TC S 7006; TCS 7006; Tpl2 Kinase Inhibitor;

IUPAC/Chemical Name: 4-[(3-Chloro-4-fluorophenyl)amino]-6-[(3-pyridinylmethyl)amino]-1,7-naphthyridine-3-carbonitrile

InChi Key: NMEUKWOOQOHUNA-UHFFFAOYSA-N

InChi Code: InChI=1S/C21H14ClFN6/c22-17-6-15(3-4-18(17)23)29-21-14(8-24)11-26-19-12-28-20(7-16(19)21)27-10-13-2-1-5-25-9-13/h1-7,9,11-12H,10H2,(H,26,29)(H,27,28)

SMILES Code: N#CC1=C(NC2=CC=C(F)C(Cl)=C2)C3=CC(NCC4=CC=CN=C4)=NC=C3N=C1

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

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

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 404.83 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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Chorzalska A, Ahsan N, Rao RSP, Roder K, Yu X, Morgan J, Tepper A, Hines S, Zhang P, Treaba DO, Zhao TC, Olszewski AJ, Reagan J, Liang O, Gruppuso PA, Dubielecka PM. Overexpression of Tpl2 is linked to imatinib resistance and activation of MEK-ERK and NF-κB pathways in a model of Chronic Myeloid Leukemia. Mol Oncol. 2018 Feb 27. doi: 10.1002/1878-0261.12186. [Epub ahead of print] PubMed PMID: 29485707.

2: Senger K, Pham VC, Varfolomeev E, Hackney JA, Corzo CA, Collier J, Lau VWC, Huang Z, Hamidzhadeh K, Caplazi P, Peng I, Setiadi AF, Francis R, Paler-Martinez A, Kwon YC, Ramirez-Carrozzi V, Sun Y, Grigg PW, Roose-Girma M, Jeet S, Barck KH, Pham A, Ota N, Ha C, Stinson J, Guillory J, Tam L, Modrusan Z, Emson C, McKenzie BS, Townsend MJ, Carano RAD, Warming S, Vucic D, DeVoss J, Lee WP, Lill JR, Zarrin AA. The kinase TPL2 activates ERK and p38 signaling to promote neutrophilic inflammation. Sci Signal. 2017 Apr 18;10(475). pii: eaah4273. doi: 10.1126/scisignal.aah4273. PubMed PMID: 28420753.

3: Jang S, Kim J, Cha JH. Cot kinase plays a critical role in Helicobacter pylori-induced IL-8 expression. J Microbiol. 2017 Apr;55(4):311-317. doi: 10.1007/s12275-017-7052-9. Epub 2017 Mar 31. PubMed PMID: 28361341.

4: Vyrla D, Nikolaidis G, Oakley F, Perugorria MJ, Tsichlis PN, Mann DA, Eliopoulos AG. TPL2 Kinase Is a Crucial Signaling Factor and Mediator of NKT Effector Cytokine Expression in Immune-Mediated Liver Injury. J Immunol. 2016 May 15;196(10):4298-310. doi: 10.4049/jimmunol.1501609. Epub 2016 Apr 6. PubMed PMID: 27053764.

5: Sharma V, Young L, Cavadas M, Owen K; Reproducibility Project: Cancer Biology. Registered Report: COT drives resistance to RAF inhibition through MAP kinase pathway reactivation. Elife. 2016 Mar 21;5. pii: e11414. doi: 10.7554/eLife.11414. PubMed PMID: 26999821; PubMed Central PMCID: PMC4811761.

6: Kaniaris E, Vaporidi K, Vergadi E, Theodorakis EE, Kondili E, Lagoudaki E, Tsatsanis C, Georgopoulos D. Genetic and pharmacologic inhibition of Tpl2 kinase is protective in a mouse model of ventilator-induced lung injury. Intensive Care Med Exp. 2014 Dec;2(1):15. doi: 10.1186/2197-425X-2-15. Epub 2014 May 9. PubMed PMID: 26266915; PubMed Central PMCID: PMC4513004.

7: Kuriakose T, Rada B, Watford WT. Tumor progression locus 2-dependent oxidative burst drives phosphorylation of extracellular signal-regulated kinase during TLR3 and 9 signaling. J Biol Chem. 2014 Dec 26;289(52):36089-100. doi: 10.1074/jbc.M114.587121. Epub 2014 Nov 5. PubMed PMID: 25378393; PubMed Central PMCID: PMC4276873.

8: Kanellis DC, Bursac S, Tsichlis PN, Volarevic S, Eliopoulos AG. Physical and functional interaction of the TPL2 kinase with nucleophosmin. Oncogene. 2015 May 7;34(19):2516-26. doi: 10.1038/onc.2014.183. Epub 2014 Jul 7. PubMed PMID: 24998852.

9: Chowdhury FZ, Estrada LD, Murray S, Forman J, Farrar JD. Pharmacological inhibition of TPL2/MAP3K8 blocks human cytotoxic T lymphocyte effector functions. PLoS One. 2014 Mar 18;9(3):e92187. doi: 10.1371/journal.pone.0092187. eCollection 2014. PubMed PMID: 24642963; PubMed Central PMCID: PMC3958505.

10: Kusuyama J, Bandow K, Shamoto M, Kakimoto K, Ohnishi T, Matsuguchi T. Low intensity pulsed ultrasound (LIPUS) influences the multilineage differentiation of mesenchymal stem and progenitor cell lines through ROCK-Cot/Tpl2-MEK-ERK signaling pathway. J Biol Chem. 2014 Apr 11;289(15):10330-44. doi: 10.1074/jbc.M113.546382. Epub 2014 Feb 18. PubMed PMID: 24550383; PubMed Central PMCID: PMC4036157.

11: Kim G, Khanal P, Kim JY, Yun HJ, Lim SC, Shim JH, Choi HS. COT phosphorylates prolyl-isomerase Pin1 to promote tumorigenesis in breast cancer. Mol Carcinog. 2015 Jun;54(6):440-8. doi: 10.1002/mc.22112. Epub 2013 Nov 22. PubMed PMID: 24265246.

12: Lee BK, Chung MY, Lee KW. Benzo[a]pyrene-7,8-diol-9,10-epoxide inhibits gap junction intercellular communication via phosphorylation of tumor progression locus 2 in WB-F344 rat liver epithelial cells. Mol Carcinog. 2015 May;54(5):351-8. doi: 10.1002/mc.22103. Epub 2013 Nov 19. PubMed PMID: 24249418.

13: Hirschhorn J, Mohanty S, Bhat NR. The role of tumor progression locus 2 protein kinase in glial inflammatory response. J Neurochem. 2014 Mar;128(6):919-26. doi: 10.1111/jnc.12522. Epub 2013 Nov 21. PubMed PMID: 24188160; PubMed Central PMCID: PMC3951670.

14: Decicco-Skinner KL, Jung SA, Tabib T, Gwilliam JC, Alexander H, Goodheart SE, Merchant AS, Shan M, Garber C, Wiest JS. Tpl2 knockout keratinocytes have increased biomarkers for invasion and metastasis. Carcinogenesis. 2013 Dec;34(12):2789-98. doi: 10.1093/carcin/bgt319. Epub 2013 Sep 25. PubMed PMID: 24067898; PubMed Central PMCID: PMC3845897.

15: Lee WJ, Lan KH, Chou CT, Yi YC, Chen WC, Pan HC, Peng YC, Wang KB, Chen YC, Chao TH, Tien HR, Sheu WH, Sheu ML. Tpl2 inhibitors thwart endothelial cell function in angiogenesis and peritoneal dissemination. Neoplasia. 2013 Sep;15(9):1036-48. PubMed PMID: 24027429; PubMed Central PMCID: PMC3769883.

16: Lee HW, Joo KM, Lim JE, Cho HJ, Cho HJ, Park MC, Seol HJ, Seo SI, Lee JI, Kim S, Jeong BC, Nam DH. Tpl2 kinase impacts tumor growth and metastasis of clear cell renal cell carcinoma. Mol Cancer Res. 2013 Nov;11(11):1375-86. doi: 10.1158/1541-7786.MCR-13-0101-T. Epub 2013 Aug 27. PubMed PMID: 23982215.

17: Pan HC, Lai DW, Lan KH, Shen CC, Wu SM, Chiu CS, Wang KB, Sheu ML. Honokiol thwarts gastric tumor growth and peritoneal dissemination by inhibiting Tpl2 in an orthotopic model. Carcinogenesis. 2013 Nov;34(11):2568-79. doi: 10.1093/carcin/bgt243. Epub 2013 Jul 4. PubMed PMID: 23828905.

18: Martel G, Bérubé J, Rousseau S. The protein kinase TPL2 is essential for ERK1/ERK2 activation and cytokine gene expression in airway epithelial cells exposed to pathogen-associated molecular patterns (PAMPs). PLoS One. 2013;8(3):e59116. doi: 10.1371/journal.pone.0059116. Epub 2013 Mar 19. PubMed PMID: 23527104; PubMed Central PMCID: PMC3602461.

19: DeCicco-Skinner KL, Nolan SJ, Deshpande MM, Trovato EL, Dempsey TA, Wiest JS. Altered prostanoid signaling contributes to increased skin tumorigenesis in Tpl2 knockout mice. PLoS One. 2013;8(2):e56212. doi: 10.1371/journal.pone.0056212. Epub 2013 Feb 15. PubMed PMID: 23457529; PubMed Central PMCID: PMC3574127.

20: Kim G, Khanal P, Lim SC, Yun HJ, Ahn SG, Ki SH, Choi HS. Interleukin-17 induces AP-1 activity and cellular transformation via upregulation of tumor progression locus 2 activity. Carcinogenesis. 2013 Feb;34(2):341-50. doi: 10.1093/carcin/bgs342. Epub 2012 Nov 3. PubMed PMID: 23125217.