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.
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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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
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.
In Vivo
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.
Protocols
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Ibt-DOX Related Classifications
HY-181546 Related Classifications
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