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Tocris/TC-S 7006/5240/10/10 mg

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货号: 5240/10

品牌: Tocris

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Description: Potent and selective Tpl2 (Cot; MAP3K8) inhibitor

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

Purity: ≥99% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Potent and selective Tpl2 (Cot; MAP3K8) inhibitor (IC₅₀ = 50 nM). Selective for Tpl2 over MEK, p38, Src, MK2, PKC and EGFR. Inhibits LPS-induced TNF-α secretion from monocytes and attenuates acute myeloid leukemia (AML) cell proliferation in vitro. Also reduces cytolytic activity of human CD8⁺ cytotoxic T lymphocytes. Cell permeable.

Compound Libraries

TC-S 7006 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	404.83
Formula	C₂₁H₁₄ClFN₆
Storage	Store at -20°C
Purity	≥99% (HPLC)
CAS Number	871307-18-5
PubChem ID	9549300
InChI Key	NMEUKWOOQOHUNA-UHFFFAOYSA-N
Smiles	FC(C(Cl)=C4)=CC=C4NC1=C2C(C=NC(NCC3=CN=CC=C3)=C2)=NC=C1C#N

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	40.48	100

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 solvent 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	2.47 mL	12.35 mL	24.7 mL
5 mM	0.49 mL	2.47 mL	4.94 mL
10 mM	0.25 mL	1.24 mL	2.47 mL
50 mM	0.05 mL	0.25 mL	0.49 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Chowdhury et al (2014) Pharmacological inhibition of TPL2/MAP3K8 blocks human cytotoxic T lymphocyte effector functions. PLoS ONE 9 e92187 PMID: 24642963

Wang et al (2010) Inhibition of Cot1/Tlp2 oncogene in AML cells reduces ERK5 activation and up-regulates p27^Kip1 concomitant with enhancement of differentiation and cell cycle arrest induced by silibinin and 1,25-dihydroxyvitamin D₃. Cell Cycle 9 4542 PMID: 21084834

Gavrin et al (2005) Inhibition of Tpl2 kinase and TNF-α production with 1,7-naphthyridine-3-carbonitriles: synthesis and structure-activity relationships. Bioorg.Med.Chem.Lett. 15 5288 PMID: 16165349

Keywords: TC-S 7006, supplier, TC-S7006, potent, selective, TPL2, Cot, MAP3K8, inhibits, inhibitors, Other, Kinases, Other, Kinases, Tocris Bioscience

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