Ibt-DOX
Ibt-DOX is a BTK inhibitor with an IC50 of 2.89 nM. Ibt-DOX is also a targeted covalent activated chemotherapeutic agent composed of the targeting ligand Ibrutinib (HY-10997), Doxorubicin (DOX) (HY-15142A), α-MAA (HY-W017180), and a linker (HY-Y0892). Ibt-DOX specifically binds to BTK and releases DOX, synergistically achieving BTK inhibition and chemotherapeutic killing, significantly enhancing toxicity against B-cell lymphoma cells and greatly reducing the toxic side effects of DOX on BTK-negative cells. Ibt-DOX can be used in lymphoma-related research.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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。
- 分子式: C61H59N7O16
- 分子量:1146.16
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
体外実験
Ibt-DOX (25-50 nM; 1 h) specifically releases free DOX in BTK-expressing OCI-LY10 cells, but exerts no such effect in BTK-negative Jurkat cells[1].
Ibt-DOX (0-1000 nM; 1 h) potently inhibits the BTK-mediated BCR signaling pathway in OCI-LY10 cells, it completely blocks the phosphorylation of BTK and its downstream effector molecules at a concentration of 75 nM[1].
Ibt-DOX (0-400 nM; 20 h) induces significant release of extracellular ATP and HMGB1 in BTK-expressing OCI-LY10 cells, but exerts no such effect in BTK-negative Jurkat cells[1].
Ibt-DOX (0-100 μM; 72 h) exhibits potent antiproliferative activity against BTK-expressing OCI-LY10 and Ramos cells, while its activity is significantly reduced in BTK-negative cells, demonstrating selective cytotoxicity toward BTK-expressing B-cell lymphoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:OCI-LY10
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Concentration:75 nM
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Incubation Time:1 h
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Result:Completely inhibited phosphorylation of BTK, PLCγ2, and Erk1/2.
Left phosphorylation of upstream kinase Syk unaffected.
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Cell Line:OCI-LY10, Ramos, Jurkat, MCF-7, HepG2, HL-7702
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Concentration:0-100 μM
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Incubation Time:72 h
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Result:Achieved an IC50 of 0.206 μM in OCI-LY10 cells.
Achieved an IC50 of 0.231 μM in Ramos cells.
Achieved an IC50 of 7.1 μM in Jurkat cells.
Achieved an IC50 of 17.9 μM in MCF-7 cells.
Achieved an IC50 of 52.3 μM in HepG2 cells.
Achieved an IC50 of 28.4 μM in HL-7702 cells.
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:SCID mice treated OCI-LY10 cells (female)[1]
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Dosage:2.5 mg/kg
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Administration:i.v.; once every 2 days; 14 days
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Result:Reduced average tumor size by 54% compared to the vehicle group.
Showed no significant body weight change or poisoning symptoms.
化学情報
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分子量 1146.16
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分子式 C61H59N7O16
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SMILES
NC1=C(C(C2=CC=C(C=C2)OC3=CC=CC=C3)=NN4[C@@H]5CCCN(C5)C(C(COC6=CC=C(C=C6)COC(N[C@H]7C[C@@H](O[C@@H](C)[C@H]7O)O[C@H]8C[C@@](O)(CC9=C8C(O)=C%10C(C(C%11=C(C%10=O)C(OC)=CC=C%11)=O)=C9O)C(CO)=O)=O)=C)=O)C4=NC=N1
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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.
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)
Ibt-DOX 関連分類
HY-181546 関連分類
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