1. Protein Tyrosine Kinase/RTK
  2. Btk
  3. PROTAC BTK Degrader-5

PROTAC BTK Degrader-5 (compound 3e) 是一种具有选择性的 BTK 降解剂,对 JeKo-1 细胞的 DC50 值为 7.0 nM。PROTAC BTK Degrader- 5对 CRBN 新基态无脱靶效应。PROTAC BTK Degrader-5 对淋巴瘤细胞具有抗增殖作用,可用于恶性淋巴瘤研究1

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PROTAC BTK Degrader-5 Chemical Structure

PROTAC BTK Degrader-5 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PROTAC BTK degraders-5(compound 3e) is a selective BTK degrader with a DC50 value of 7.0 nM in JeKo-1 cells. PROTAC BTK degraders-5 has no off-target effect on degrading CRBN neosubstates. PROTAC BTK degraders-5 has anti-proliferation effect on various lymphoma tumor cells and can be used in chronic lymphoid malignancies research1.

体外研究
(In Vitro)

PROTAC BTK Degrader-5 (Compound 3e) (1.6~1000 nM; 24 h) 诱导 JeKo-1 细胞中 BTK 的降解,DC50 值为7.0 nM[1]
PROTAC BTK Degrader-5 (100 and 1000 nM) 具有代谢稳定性,其半衰期为 145 分钟[1]
PROTAC BTK Degrader-5 (100 nM;12 h) 诱导的 BTK 降解被蛋白酶体抑制剂 MG - 132 (HY-13259) (5.0 μM) 有效阻断[1]
PROTAC BTK Degrader-5 (1.6~1000 nM; 24 h)对 IKZF1 和 GSPT1 无降解作用,对 IKZF3 有一定的降解作用[1]
PROTAC BTK Degrader-5 (72 h) 对OCI-ly10、TMD8、JeKo-1、BTKC481S Ba/F3细胞具有抗增殖作用, IC50 值分别为 2.3、4.5、38.1 和 86.0 nM,效果高于 Ibrutinib (HY-10997) (IC50 分别为 4.5、4.7、79.8 和 1546.0 nM)[1]

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

体内研究
(In Vivo)

PROTAC BTK Degrader-5(2 mg/kg, 静脉注射, 单剂量)在小鼠体内代谢稳定[1]

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

Animal Model: The male Balb/c mice[1]
Dosage: a single dose 2 mg/kg or 100 mg/kg, 5% DMSO, 10% Solutol, 85% saline
Administration: Intravenous injection (i.v.); Oral gavage (p.o.)
Result: Maintained above 10 nM for at least 4 h after administration of PROTAC BTK Degrader-5 at a single dose of 2 mg/kg via intravenous (IV) injection in the plasma (the effective BTK degradation DC5050 = 7.0nM).
Had poor oral bioavailability at a dose of 100 mg/kg.
分子量

958.52

Formula

C52H57ClFN9O6

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

PROTAC BTK Degrader-5 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 *
= × ×

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.

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产品名称:
PROTAC BTK Degrader-5
目录号:
HY-155072
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