2. Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage
  3. Btk PERK Syk HMG Family
  4. 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.

Ibt-DOX

Ibt-DOX Chemical Structure

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Ibt-DOX Related Antibodies

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Description

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[1].

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.

Ibt-DOX Related Antibodies

Western Blot Analysis[1]

Cell Line: OCI-LY10
Concentration: 75 nM
Incubation Time: 1 h
Result: Completely inhibited phosphorylation of BTK, PLCγ2, and Erk1/2.
Left phosphorylation of upstream kinase Syk unaffected.

Cell Proliferation Assay[1]

Cell Line: OCI-LY10, Ramos, Jurkat, MCF-7, HepG2, HL-7702
Concentration: 0-100 μM
Incubation Time: 72 h
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

Ibt-DOX (2.5 mg/kg; i.v.; once every 2 days; 14 days) reduces OCI-LY10 xenograft tumor volume by 54% in SCID mice with good tolerability[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice treated OCI-LY10 cells (female)[1]
Dosage: 2.5 mg/kg
Administration: i.v.; once every 2 days; 14 days
Result: Reduced average tumor size by 54% compared to the vehicle group.
Showed no significant body weight change or poisoning symptoms.
Molecular Weight

1146.16

Formula

C61H59N7O16
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Ibt-DOX Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ibt-DOXBtkPERKSykHMG FamilyBruton tyrosine kinaseProtein kinase R-like endoplasmic reticulum kinasePKR-like endoplasmic reticulum kinaseSpleen tyrosine kinaseHigh Mobility Group FamilyB-cell lymphoma cellsBTKOCI-LY10 cellsErk1/2PLCγ2BCR signalingRamos cellsJurkat cellsInhibitorinhibitorinhibit

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