2. Protein Tyrosine Kinase/RTK Apoptosis Cell Cycle/DNA Damage Epigenetics
  3. Btk Caspase Apoptosis PARP
  4. BTK-IN-47

BTK-IN-47 (Compound 9e) 是一种共价的、选择性的 BTK 抑制剂，对 BTK 的 IC50 为 5.15 nM。BTK-IN-47 抑制 BTK 信号通路、诱导细胞周期阻滞，并激活经典的 Caspase 依赖性凋亡 (Apoptotic) 通路 (促进 Caspase-3、Caspase-7 和 PARP 的裂解)，且不会诱导坏死性凋亡、焦亡或铁死亡。BTK-IN-47 对血液肿瘤细胞系具有剂量依赖性的抗增殖活性。BTK-IN-47 在 BALB/c 裸鼠的 Ramos 细胞异种移植模型中具有剂量依赖性的体内抗肿瘤活性。BTK-IN-47 可用于血液肿瘤的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

BTK-IN-47

BTK-IN-47 Chemical Structure

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

BTK-IN-47 相关抗体

Top Publications Citing Use of Products

查看 Caspase 亚型特异性产品:

查看所有亚型
Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

查看 PARP 亚型特异性产品:

查看所有亚型
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BTK-IN-47 (Compound 9e) is a covalent, selective BTK inhibitor with an IC50 of 5.15 nM against BTK. BTK-IN-47 inhibits the BTK signaling pathway, induces cell cycle arrest, and activates the canonical Caspase-dependent Apoptotic pathway (promoting the cleavage of Caspase-3, Caspase-7 and PARP), without inducing necroptosis, pyroptosis or ferroptosis. BTK-IN-47 exerts dose-dependent antiproliferative activity against hematologic tumor cell lines. BTK-IN-47 exhibits dose-dependent in vivo antitumor activity in a Ramos cell xenograft model in BALB/c nude mice. BTK-IN-47 can be used for the research of hematologic malignancies[1].

IC50 & Target[1]

Caspase 3

 

Caspase-7

 

体外研究
(In Vitro)

BTK-IN-47 可在体外强效抑制重组 BTK 激酶活性，其 IC50 为 5.15 nM[1]。
BTK-IN-47 (48 h) 可在体外抑制 Ramos、Raji、MOLM-13 和 Jurkat 血液肿瘤细胞系的增殖，其 IC50 值为 2.04 至 4.03 μM[1]。
BTK-IN-47 (1-10 μM; 48 h) 可在体外以剂量依赖方式诱导 Ramos 细胞发生 G1 期细胞周期阻滞和 caspase 介导的细胞凋亡，且不会激活坏死性凋亡、焦亡或铁死亡通路[1]。

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

BTK-IN-47 相关抗体:

Cell Proliferation Assay[1]

Cell Line: Ramos, Raji, MOLM-13, Jurkat hematological tumor cell lines
Concentration: Serial dilutions
Incubation Time: 48 h
Result: Exhibited antiproliferative activity with IC50 values of 2.68 ± 0.54 μM (Ramos), 2.04 ± 1.51 μM (Raji), 2.73 ± 0.17 μM (MOLM-13), and 4.03 ± 0.43 μM (Jurkat).

Apoptosis Analysis[1]

Cell Line: Ramos cells
Concentration: 1-10 μM
Incubation Time: 48 h
Result: Induced apoptosis with rates of 30.7% (1 μM) and 37.5% (10 μM), and facilitated cleavage of Caspase-3, Caspase-7, and PARP.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax AUC0-t AUC0-∞ Vz CL Bioavailability
Rat[1] 1 mg/kg i.v. 9.75 ± 2.46 h 41.82 ± 4.71 μg/L 161.45 ± 59.89 μg/L·h 190.46 ± 71.62 μg/L·h 80.43 ± 36.64 L/kg 5.70 ± 1.79 L/h/kg /
Rat[1] 10 mg/kg p.o. 2.74 ± 1.00 h 87.31 ± 32.80 μg/L 190.97 ± 19.36 μg/L·h 192.74 ± 22.35 μg/L·h 20.14 ± 4.96 L/kg 5.23 ± 0.57 L/h/kg 11.83 %
体内研究
(In Vivo)

BTK-IN-47 (15-30 mg/kg；注射；每日一次；连续 14 天) 对 Ramos 细胞异种移植物表现出剂量依赖性的体内抗肿瘤效果，同时可抑制 BTK 信号通路[1]。

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

Animal Model: BALB/c nude (female, 6 to 8 weeks old, subcutaneous xenograft of Ramos cells)[1]
Dosage: 15 mg/kg/day; 30 mg/kg/day
Administration: injected; daily; 14 days
Result: Achieved 82.3% tumor growth inhibition rate and reduced Ki-67 labeling index to a level comparable to ibrutinib at 15 mg/kg/day.
Achieved 87.5% tumor growth inhibition rate, significantly reduced phosphorylation of BTK and PLCγ2 in tumor tissue, and lowered Ki-67 labeling index to 41.60% at 30 mg/kg/day.
Caused no significant body weight loss or systemic tissue damage at either dose.
分子量

490.56

Formula

C28H26N8O
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

BTK-IN-47 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:

BTK-IN-47BtkCaspaseApoptosisPARPBruton tyrosine kinasepoly ADP ribose polymeraseRamos cell xenograft modelG0/G1 phase cell cycle arrestBTK-C481S mutant cellsB-cell receptor signaling pathwayhematological tumor cell linesBALB/c nude miceBruton's tyrosine kinaseBTK Cys481caspase-dependent apoptotic pathwaySprague-Dawley ratsInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
BTK-IN-47
目录号：
HY-181996
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z