ALK-IN-12
ALK-IN-12 is a potent and orally active ALK inhibitor with an IC50 of 0.18 nM. ALK-IN-12 also inhibits IGF1R and InsR (IC50=20.3 and 90.6 nM). Antitumor activities.
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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: 1197958-53-4
- 分子式: C24H30ClN6O2P
- 分子量:500.96
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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
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| KARPAS-299 | IC50 |
28.3 nM
Compound: 11e
|
Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
Antiproliferative activity against human ALK-positive KARPAS299 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
|
[PMID: 27144831] |
| U-937 | IC50 |
1590 nM
Compound: 11e
|
Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
Antiproliferative activity against human ALK-negative U937 cells assessed as reduction in cell viability measured after 72 hrs by CellTiter 96 aqueous one solution cell proliferation assay
|
[PMID: 27144831] |
ALK-IN-12 (compound 11e) effectively inhibits viability of the Karpas-299 ALCL cell line with an IC50 of 28.3 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
ALK-IN-12 (3 mg/kg; i.v.; 6-8 week old female CD rats ) treatment shows AUC0-∞, CL, t1/2 and Vss are 3039 ng h/mL, 0.91 h kg, 6.6 hours and 6.12 L/kg, respectively[1].
ALK-IN-12 (10 mg/kg; p.o.; 6-8 week old female CD rats) treatment shows Cmax, AUC0-∞, tmax, t1/2 and F are 3254 ng/mL, 4056 ng h/mL, 6.0 hours, 12.5 hours and 39%, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Eight- to 10-week old female SCID/beige mice (Karpas-299 xenograft mouse model expressing the NPM-ALK fusion)[1]
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Dosage:10-50 mg/kg
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Administration:Orally; once daily for 13 consecutive days
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Result:Dose-dependent antitumor activity. Led to tumor stasis (50 mg/kg dose).
化学情報
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CAS 番号 1197958-53-4
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分子量 500.96
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分子式 C24H30ClN6O2P
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SMILES
CN1CCN(C2=CC=C(NC3=NC=C(Cl)C(NC4=CC=CC=C4P(C)(C)=O)=N3)C(OC)=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.
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)