TAK-715

Alias: TAK 715; TAK715; TAK-715
Cat No.:V0487 Purity: ≥98%
TAK-715 is a novel, potent and selective p38 MAPK (p38 mitogen-activated protein) inhibitorwith potential anti-inflammatory activity.
TAK-715 Chemical Structure CAS No.: 303162-79-0
Product category: p38 MAPK
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

TAK-715 is a novel, potent and selective p38 MAPK (p38 mitogen-activated protein) inhibitor with potential anti-inflammatory activity. It has an IC50 of 7.1 nM, is 28-fold more selective for p38 than p38, and exhibits little to no inhibition of JNK1, ERK1, IKK, MEKK1, or TAK1. It also shows little to no inhibition of p38γ/δ, and inhibits p38α only. For the treatment of Rheumatoid arthritis-RA, TAK-715 is currently being studied in clinical trials.

Biological Activity I Assay Protocols (From Reference)
Targets
p38α (IC50 = 7.1 nM); p38β (IC50 = 200 nM); p38δ (IC50 >10 μM); p38γ (IC50 >10 μM); CK1δ; CK1ε
ln Vitro
TAK 715 has an IC50 of 48 nM and inhibits LPS-stimulated TNF-alpha release from THP-1. [1] Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift in U2OS-EFC cells are inhibited by TAK 715 (10 μM).[2] The main-chain carbonyl of Met109 of p38 alpha is hydrogen bonded to the amide NH of TAK 715. TAK 715 occupies the hydrophobic back pocket, the adenine region, the front pocket of p38, as well as the majority of the length of the Gly-rich loop, and binds relatively high in the ATP pocket.[3]
ln Vivo
TAK 715 (10 mg/kg, po) reduces the amount of TNF-alpha produced by LPS in mice by 87.6%. TAK 715 has a modest bioavailability in mice of 18.4% and a marginally better bioavailability in rats of 21.1%. TAK 715 has a modest bioavailability in mice of 18.4% and a marginally better bioavailability in rats of 21.1%. Rats treated with TAK 715 have a Cmax of 0.19 μg/mL and an AUC(0-24 hours) of 1.16 μg/h/mL. In a rat adjuvant-induced arthritis (AA) model, TAK 715 (30 mg/kg, po) significantly lowers the secondary paw volume with 25% inhibition. [1]
Enzyme Assay
TAK-715 is a p38α MAPK inhibitor with an IC50 of 7.1 nM that is 28-fold more selective for p38α over p38β, with no inhibition to p38γ/δ, JNK1, ERK1, IKKβ, MEKK1 or TAK1.
Cell Assay
TAK 715 has an IC50 of 48 nM and inhibits LPS-stimulated TNF-alpha release from THP-1. In U2OS-EFC cells, TAK 715 (10 μM) prevents Wnt-3a-induced hDvl2 phosphorylation and the hDvl2 shift. The main-chain carbonyl of Met109 of p38 alpha is hydrogen bonded to the amide NH of TAK 715. TAK 715 occupies the hydrophobic back pocket, the adenine region, the front pocket of p38, as well as the majority of the length of the Gly-rich loop, and binds relatively high in the ATP pocket.
Animal Protocol
Adjuvant-induced arthritis (AA) rat model
30 mg/kg
Orally
References

[1]. J Med Chem . 2005 Sep 22;48(19):5966-79.

[2]. Chem Biol . 2011 Apr 22;18(4):485-94.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H21N3OS
Molecular Weight
399.51
Exact Mass
399.14
Elemental Analysis
C, 72.15; H, 5.30; N, 10.52; O, 4.00; S, 8.03
CAS #
303162-79-0
Appearance
Light to dark yellow solid powder
SMILES
CCC1=NC(=C(S1)C2=CC(=NC=C2)NC(=O)C3=CC=CC=C3)C4=CC=CC(=C4)C
InChi Key
HEKAIDKUDLCBRU-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H21N3OS/c1-3-21-27-22(18-11-7-8-16(2)14-18)23(29-21)19-12-13-25-20(15-19)26-24(28)17-9-5-4-6-10-17/h4-15H,3H2,1-2H3,(H,25,26,28)
Chemical Name
N-[4-[2-ethyl-4-(3-methylphenyl)-1,3-thiazol-5-yl]pyridin-2-yl]benzamide
Synonyms
TAK 715; TAK715; TAK-715
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: ~80 mg/mL (~200.2 mM)
Water: <1 mg/mL
Ethanol: ~16 mg/mL (~40.0 mM)
Solubility (In Vivo)
30% propylene glycol, 5% Tween 80, 65% D5W: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.5031 mL 12.5153 mL 25.0307 mL
5 mM 0.5006 mL 2.5031 mL 5.0061 mL
10 mM 0.2503 mL 1.2515 mL 2.5031 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00760864 Completed Drug: TAK-715 and methotrexate
Drug: Methotrexate
Arthritis, Rheumatoid Takeda August 2004 Phase 2
Biological Data
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