2. Protein Tyrosine Kinase/RTK
  3. DYRK
  4. TSL2109

TSL2109 是一种口服有效的、选择性 DYRK2 和 CDK4/6 抑制剂，其对 DYRK2 的 IC50 值为 22 nM，激酶选择性高于 93%。TSL2109在体外诱导细胞周期阻滞并促进细胞凋亡 (apoptosis)。TSL2109 通过抑制体内外肿瘤生长，有效克服 Enzalutamide (HY-70002) 耐药性。TSL2109 展现细胞周期蛋白依赖性激酶 4/6 (CDK4/6) 抑制剂的耐药性。TSL2109 展现出良好的安全性。TSL2109 可用于前列腺癌和乳腺癌的研究[1][2].

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

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

TSL2109

TSL2109 Chemical Structure

CAS No. : 2619847-12-8

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

TSL2109 相关抗体

Top Publications Citing Use of Products

查看 DYRK 亚型特异性产品:

查看所有亚型
DYRK1 DYRK2 DYRK3 DYRK4 HIPK PRP4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

TSL2109 is an orally active and selective DYRK2 and CDK4/6 inhibitor with an IC50 value of 22 nM for DYRK2. TSL2109 exhibits high kinase selectivity over 93%. TSL2109 arrests cell cycle and induces apoptosis in virto. TSL2109 effectively overcomes Enzalutamide (HY-70002) resistance by suppressing tumor growth in vivo and virto. TSL2109 also shows CDK4/6 inhibitor resistance.TSL2109 demonstrates safety profile. TSL2109 can be used for prostate cancer research and breast cancer[1][2].
体外研究
(In Vitro)

TSL2109 (0.5-2 μM，处理72 h-5 天) 在前列腺癌 DU145 细胞中表现出强效的抗增殖活性 (IC50 = 0.933 μM) 和剂量依赖性的细胞生长抑制作用[1]。
TSL2109 (0.5-2 μM，处理 24 小时) 在 DU145 细胞中诱导 G1 期细胞周期阻滞并促进细胞凋亡，在22Rv1 细胞中显著抑制增殖，诱导明显的 G1 期细胞周期阻滞，并促进细胞凋亡[1]。
TSL2109 在 DU145 细胞和 22Rv1 细胞中显著抑制 E2F 靶基因通路和 G2/M 检查点通路，并在DU145 细胞中上调凋亡通路和 P53 通路[1]。
TSL2109 (50 或 100 μM，处理 7 天) 在 Enzalutamide (HY-70002) 耐药的前列腺癌类器官模型 (PDOs) (PR6513B) 中表现出优异的生长抑制作用[1]。
TSL2109 能显著抑制雄激素受体 (AR) 抑制剂耐药的前列腺癌细胞及类器官的增殖[2]。
TSL2109 可下调磷酸化视网膜母细胞瘤蛋白 (p-RB)、磷酸化 4E 结合蛋白 1 (p-4E-BP1) 及 B 细胞淋巴瘤因子 2 (BCL2) 的表达[2]。
TSL2109 能显著抑制 E2F 信号通路及 G2/M 期相关信号通路的活性[2]。

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

TSL2109 相关抗体:

Cell Viability Assay[1]

Cell Line: PCa DU145 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 5 days
Result: Shows a dose-dependent cell growth inhibitory activity.

Cell Cycle Analysis[1]

Cell Line: DU145 and 22Rv1 cell cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Arrested cell cycle at G1 phase in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: DU145 and 22Rv1 cells
Concentration: 0.5, 1, 2 μM
Incubation Time: 24 h
Result: Promoted apoptosis in a concentration-dependent manner.

Cell Proliferation Assay[1]

Cell Line: 22Rv1 and DU145 cell
Concentration: 0.5, 1, 2 μM
Incubation Time: 72 h
Result: Exerted significant inhibitory effects on 22Rv1 cell proliferation.
体内研究
(In Vivo)

TSL2109 (100-200 mg/kg，口服灌胃，每日一次，持续 45 天) 在 DU145 小鼠异种移植瘤模型中显示出良好的安全性[1]。
TSL2109 (1000 mg/kg，口服灌胃，单次给药) 在DU145小鼠异种移植瘤模型中具有优异的耐受性与安全性且未引起不良行为学效应[1]。
TSL2109 (75 mg/kg，口服灌胃，每日一次，持续 21 天) 展现出克服 Enzalutamide 耐药性的潜力，并有望增强 Enzalutamide 的疗效[1]。
TSL2109 (100 mg/kg，每日一次，持续 30 天) 在 Enzalutamide 耐药PDX小鼠模型中显示出克服 Enzalutamide 耐药性的潜力[1]。
TSL2109 可有效抑制 AR 抑制剂耐药的前列腺癌 PDX 模型的肿瘤生长[2]。
TSL2109 在 CDK4/6 抑制剂耐药的乳腺癌模型中表现出强效的活性[2]。

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

Animal Model: DU145 cell induced-Male BALB/c nude mice[1]
Dosage: 1000 mg/kg
Administration: o.p, once
Result: Exhibited normal body weight gain.
Caused no adverse behavioral effects during a 48 h observation period.
Maintained normal weight gain over 14 days.
Observed no significant changes in the weights of major organs (heart, liver, spleen, lung, kidney) after 14 days.
Animal Model: DU145 cell induced-Male BALB/c nude mice[1]
Dosage: 100 and 200 mg/kg
Administration: o.p, once daily for 15 days
Result: Obviously inhibited 22Rv1 xenografts tumor growth.
Improved tumor growth inhibitory activity when combination with Enzalutamide.
Animal Model: PDX tissue (s.c.) induced-male NU/ NU mice[1]
Dosage: 100 mg/kg
Administration: once a day for 30 days
Result: Induced robust tumor growth suppression.
Significantly reduced tumor burden.
分子量

548.68

Formula

C28H33FN8OS
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

TSL2109 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:

TSL21092619847-12-8TSL 2109TSL-2109DYRKDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseInhibitorinhibitorinhibit

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：
TSL2109
目录号：
HY-180574
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