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.
For research use only. We do not sell to patients.
- Formula: C61H59N7O16
- Molecular Weight:1146.16
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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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.
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.
Chemical Information
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Molecular Weight 1146.16
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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