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

PROTAC BTK Degrader-1 是一种有效且具有选择性和口服活性的 PROTAC BTK 降解剂，对野生型 BTK 和突变型 BTK-481S 的IC50 分别为 34.51 nM 和 64.56 nM。PROTAC BTK Degrader-1 能有效降低 BTK 蛋白水平，抑制肿瘤生长。

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PROTAC BTK Degrader-1 Chemical Structure

PROTAC BTK Degrader-1 Chemical Structure

CAS No. : 2801715-13-7

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PROTAC BTK Degrader-1 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

PROTAC BTK Degrader-1 is a potent, selective and orally active PROTAC BTK degrader with an IC50 value of 34.51 nM and 64.56 nM for BTK WT and BTK-481S, respectively. PROTAC BTK Degrader-1 effectively reduces BTK protein levels and suppresses tumor growth[1]. PROTAC BTK Degrader-1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

IC50: 34.51 nM (BTK WT), 64.56 nM (BTK-481S)[1]
体内研究
(In Vivo)

PROTAC BTK Degrader-1 (compound C13) (10 and 30 mg/kg; PO, bid, for 17 days) inhibits tumor growth in the OCI-ly10 xenograft mouse model[1].
Pharmacokinetic Parameters of PROTAC BTK Degrader-1 in ICR mice[1].

PO (100 mg/kg) IV (2 mg/kg)
Tmax (h) 1.00
T1/2 (h) 8.3 3.7
Cmax (ng/mL) 3089
AUC0-t (ng/mL·h) 16,894 2827
AUC0-∞ (ng/mL·h) 17,070 2845
VdSS (L/kg) 3.1
CL (mL/min/kg) 11.7
MRT (h) 4.5
F (%) 12

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

Animal Model: OCI-ly10 xenograft mouse model[1]
Dosage: 10 and 30 mg/kg
Administration: PO, bid, for 17 days
Result: Inhibited tumor growth by 50.9 and 96.9% at 10 and 30 mg/kg, respectively.
分子量

749.86

Formula

C43H43N9O4
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

PROTAC BTK Degrader-1 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.

Keywords:

PROTAC BTK Degrader-12801715-13-7PROTAC BTK Degrader1PROTAC BTK Degrader 1PROTACsBtkBruton tyrosine kinaseanticancerantitumororally activeOCI-ly10xenograftICR miceInhibitorinhibitorinhibit

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