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TAK-715

Names

[ CAS No. ]:
303162-79-0

[ Name ]:
TAK-715

[Synonym ]:
Kinome_2655
cc-467
Benzamide, N-[4-[2-ethyl-4-(3-methylphenyl)-5-thiazolyl]-2-pyridinyl]-
Benzamide, N-[3-[2-ethyl-4-(3-methylphenyl)-5-thiazolyl]-2-pyridinyl]-
N-(4-(2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl)-2-pyridyl)benzamide
N-{4-[2-Ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]pyridin-2-yl}benzamide
UNII-WE92U03C5Z
N-{4-[2-Ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridinyl}benzamide
N-{3-[2-Ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridinyl}benzamide
TAK 715
TAK-715

Biological Activity

[Description]:

TAK-715 is a p38 MAPK inhibitor for p38α with IC50 of 7.1 nM, 28-fold more selective for p38α over p38β, no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.IC50 value: 7.1 nM [1]Target: p38α MAPKin vitro: TAK 715 inhibits LPS-stimulated release of TNF-alpha from THP-1 with IC50 of 48 nM [1]. TAK 715 (10 μM) inhibits Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells [2]. The amide NH of TAK 715 is hydrogen bonded to the main-chain carbonyl of Met109 of p38 alpha. TAK 715 binds relatively high in the ATP pocket, occupying the hydrophobic back pocket, the adenine region and the front pocket of p38 as well as extending to most of the length of the Gly-rich loop [3].in vivo: TAK 715 (10 mg/kg, po) inhibits LPS-induced TNF-alpha production in mice with 87.6% inhibition. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 has a modest mouse bioavailability of 18.4% and a slightly improved rat bioavailability of 21.1%. TAK 715 results in Cmax of 0.19 μg/mL and AUC(0-24 hours) of 1.16 μg·h/mL in rats. TAK 715 (30 mg/kg, po) significantly reduces the secondary paw volume with 25 % inhibition in a rat adjuvant-induced arthritis (AA) model [1].

[Related Catalog]:

Signaling Pathways >> MAPK/ERK Pathway >> p38 MAPK
Research Areas >> Inflammation/Immunology

[References]

[1]. Miwatashi S, et al. Novel inhibitor of p38 MAP kinase as an anti-TNF-alpha drug: discovery of N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]-2-pyridyl]benzamide (TAK-715) as a potent and orally active anti-rheumatoid arthritis agent. J Med Chem, 2005, 48(19), 5966-5979.

[2]. Verkaar F, et al. Inhibition of Wnt/β-catenin signaling by p38 MAP kinase inhibitors is explained by cross-reactivity with casein kinase Iδ/?. Chem Biol, 2011, 18(4), 485-494.


[Related Small Molecules]

SB203580 | SB202190 (FHPI) | Doramapimod (BIRB 796) | LY2228820 | SB 239063 | Losmapimod | PD 169316 | Talmapimod | Tat-NR2B9c | Dehydrocorydaline chloride | VX 702 | VX-745 | SKF 86002 | Acumapimod | PH-797804

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
495.3±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C24H21N3OS

[ Molecular Weight ]:
399.508

[ Flash Point ]:
253.3±28.7 °C

[ Exact Mass ]:
399.140533

[ PSA ]:
86.61000

[ LogP ]:
4.38

[ Appearance of Characters ]:
faint yellow to dark yellow

[ Vapour Pressure ]:
0.0±1.3 mmHg at 25°C

[ Index of Refraction ]:
1.656

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
DMSO: >15mg/mL

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H319

[ Precautionary Statements ]:
P305 + P351 + P338

[ Hazard Codes ]:
Xn

[ Risk Phrases ]:
22-36

[ Safety Phrases ]:
26

[ RIDADR ]:
NONH for all modes of transport

Synthetic Route

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Precursor & DownStream

Precursor

DownStream

Related Compounds