IRAK4-IN-13
IRAK4-IN-13 (compound 21) is a potent and selective IRAK4 inhibitor with an IC50 of 0.6 nM. IRAK4-IN-13 shows high metabolic clearance with human liver microsomes (HLM) intrinsic clearance is 96 µL/min/mg.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2667681-57-2
- 分子式: C24H27N9O
- 分子量:457.53
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
IRAK4 0.6 nM (IC50) |
体外実験
IRAK4-IN-13 (compound 21) shows cell pIRAK4 potencies with an IC50 of 0.024 µM[1].
IRAK4-IN-13 (compound 21) shows selectivity with IC50s of 0.0006, 0.002, 0.044, 1.2, 0.018, 0.019, 0.082, 0.036 µM for IRAK4, IRAK1, BTK, Flt3, PI3Kδ, TRKa, TRKb, TRKc, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
化学情報
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CAS 番号 2667681-57-2
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分子量 457.53
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分子式 C24H27N9O
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SMILES
CN1CCC(N2N=CC(NC3=NC(OC4(C)CC4)=C5C(C=CC(C6=CN=CN=C6)=N5)=N3)=C2)CC1
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)