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

Ibt-DOX 是一种 BTK 抑制剂，IC50 为 2.89 nM。Ibt-DOX 也是一种靶向共价激活化疗剂，由靶向配体 Ibrutinib (HY-10997)、Doxorubicin (DOX) (HY-15142A)、α-MAA (HY-W017180) 以及连接子 (HY-Y0892) 组成。Ibt-DOX 可特异性结合 BTK 并释放 DOX，协同实现 BTK 抑制与化疗杀伤，显著提升对 B 细胞淋巴瘤细胞的毒性且大幅降低 DOX 对 BTK 阴性细胞的毒副作用。bt-DOX 可用于淋巴瘤的相关研究。

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Ibt-DOX

Ibt-DOX Chemical Structure

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Ibt-DOX 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

Ibt-DOX (25-50 nM; 1 h) 可在表达 BTK 的 OCI-LY10 细胞内特异性释放游离 Doxorubicin (DOX) (HY-15142A)，但在 BTK 阴性的 Jurkat 细胞中无此作用[1]。
Ibt-DOX (0-1000 nM; 1 h) 可强效抑制 OCI-LY10 细胞中由 BTK 介导的 BCR 信号通路，75 nM 浓度下可完全阻断 BTK 及下游效应分子的磷酸化[1]。
Ibt-DOX (0-400 nM; 20 h) 可在表达 BTK 的 OCI-LY10 细胞中诱导显著的细胞外 ATP、HMGB1 释放，但在 BTK 阴性的 Jurkat 细胞中无此作用[1]。
Ibt-DOX (0-100 μM; 72 h) 对表达 BTK 的 OCI-LY10 和 Ramos 细胞表现出强效抗增殖活性，而对 BTK 阴性细胞的活性显著降低，显示出对表达 BTK 的 B 细胞淋巴瘤细胞的选择性细胞毒性[1]。

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

Ibt-DOX 相关抗体:

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.
体内研究
(In Vivo)

Ibt-DOX (2.5 mg/kg; i.v.; once every 2 days; 14 days) 在 SCID 小鼠中可使 OCI-LY10 异种移植瘤体积降低 54%，且耐受性良好[1]。

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.
分子量

1146.16

Formula

C61H59N7O16
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Ibt-DOX 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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