2. PROTAC Protein Tyrosine Kinase/RTK
  3. PROTACs Btk
  4. TQ-3959

TQ-3959 是一种具有口服活性的 BTK PROTAC 降解剂，DC50 为 14.6 nM。TQ-3959 对野生型 BTK 和 C481S 突变体 BTK 细胞系均表现出抗增殖活性。TQ-3959 在携带 TMD-8 异种移植的雌性 NOD-SCID 小鼠中显示出肿瘤生长抑制作用。TQ-3959 可以用于B 细胞恶性肿瘤如淋巴瘤的研究。(粉色：BTK 配体：(HY-175543)，蓝色：CRBN 配体 (HY-W733888)，黑色：连接子 (HY-W061884)，E3 连接酶配体-连接子偶联物： (HY-175545))。

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TQ-3959

TQ-3959 Chemical Structure

CAS No. : 2926610-43-5

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TQ-3959 相关抗体

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TQ-3959 is an orally active BTK PROTAC degrader, with a DC50 of 14.6 nM. TQ-3959 exerts antiproliferative activity against both wild-type BTK and C481S mutant BTK cell lines. TQ-3959 exhibits tumor growth inhibition in female NOD-SCID mice bearing TMD-8 xenografts. TQ-3959 can be used in the research on B-cell malignancies such as lymphoma.(Pink: BTK ligand (HY-150885), Blue: CRBN Ligand (HY-W733888), Black: Linker (HY-W061884), E3 ligase ligand-linker conjugate (HY-175545))[1].

IC50 & Target[1]

Cereblon

 

体外研究
(In Vitro)

TQ-3959 在 OCI-Ly10 细胞中通过 HTRF 实验显示出强效的 BTK 降解活性，DC50 为 0.4 nM，Dmax 为 97.7%[1]。
TQ-3959 (72 小时) 对 OCI-Ly10 (BTK WT 细胞) (IC50 = 0.08 nM)、TMD-8 (BTK WT 细胞) (IC50 = 1.0 nM)、OCI-Ly10 (BTK C481S 细胞) (IC50 = 0.2 nM) 和 TMD-8 (BTK C481S 细胞) (IC50 = 0.6 nM) 表现出抗增殖活性[1]。

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

TQ-3959 相关抗体:
体内研究
(In Vivo)

TQ-3959 (7.5-30 mg/kg，口服，每日一次，20 天) 在携带 TMD-8 异种移植的 NOD-SCID 小鼠中显示出肿瘤生长抑制作用[1]。

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

Animal Model: TMD-8 cells (1 × 107 in 100 μL) were subcutaneously implanted into the right flanks of 6-8-week-old female NOD-SCID mice[1]
Dosage: 7.5, 15, 30 mg/kg
Administration: p.o. once daily for 20 days
Result: Achieved tumor growth inhibition (TGI) rates of 80.5%, 98.5%, and 98.8% at oral doses of 7.5, 15, and 30 mg/kg in female NOD-SCID mice bearing TMD-8 xenografts, respectively.
Showed no significant changes in body weight.
分子量

761.87

Formula

C40H47N11O5
CAS 号
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

TQ-3959 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:

TQ-39592926610-43-5TQ3959TQ 3959PROTACsBtkBruton tyrosine kinasechronic lymphocytic leukemia (CLL)MT-802BTKPROTACInhibitorinhibitorinhibit

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目录号：
HY-175541
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