HBC-12551
HBC-12551 is an orally active BTK inhibitor (IC50 in HEK293 cells: 1.31 nM for BTK; 2.18 nM for BTKC481S). HBC-12551 has antitumor activity against diffuse large B-cell lymphoma.
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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: 2963606-11-1
- 分子式: C34H41FN8O5
- 分子量:660.74
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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
体外実験
HBC-12551 potently inhibits the phosphorylation of BTK (IC50 = 1.31 nM) and the phosphorylation of the BTKC481S mutant in HEK293 cells[1].
HBC-12551 (72 h) potently reduces the cell viability of malignant B-cell lines TMD8 (IC50 = 1.40 nM), TMD8-BTK-C481S (IC50 = 1.92 nM), OCI-Ly10 (IC50 = 1.86 nM) and REC-1 (IC50 = 3.11 nM) after 72 h of incubation[1].
HBC-12551 (30 min) potently inhibits B cell activation in human peripheral blood mononuclear cells (PBMCs), with an IC50 of 0.95 nM for CD69 expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CB17 SCID (female)[1]
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Dosage:10 mg/kg; 20 mg/kg
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Administration:p.o.; QD; 14 days
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Result:Inhibited tumor growth by 97.2% relative to vehicle control.
Resulted in tumor regression with a tumor growth inhibition (TGI) of 112.8%.
Showed no abnormal clinical observations or significant body weight loss in treated mice.
化学情報
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CAS 番号 2963606-11-1
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分子量 660.74
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分子式 C34H41FN8O5
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SMILES
FC(C=C1)=CC(C(NCC(C=C2)=CC=C2N(N=C3)C(C(N)=O)=C3NC(C=C4)=NC([C@@H](C)OC)=C4N(CC5)CCN5CCOC)=O)=C1OC
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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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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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)