2. Apoptosis
  3. Apoptosis
  4. XPO1-IN-1

XPO1-IN-1 (compound D4) 是一种口服有效的 XPO1 抑制剂, 其在 MM.1S 细胞中的 IC50 为 24 nM。XPO1-IN-1 能有效诱导细胞凋亡和细胞周期阻滞。XPO1-IN-1 具有良好的代谢稳定性和药代动力学性质。XPO1-IN-1 可用于多发性骨髓瘤的研究。

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

XPO1-IN-1 Chemical Structure

XPO1-IN-1 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

XPO1-IN-1 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

XPO1-IN-1 (compound D4) is an orally active and potent XPO1 inhibitor, with an IC50 of 24 nM in MM.1S cell. XPO1-IN-1 can efficiently induce cell apoptosis and cell cycle arrest. XPO1-IN-1 displays favorable metabolic stability and pharmacokinetic properties. XPO1-IN-1 can be used for multiple myeloma (MM) research[1].

IC50 & Target

XPO1

 

体外研究
(In Vitro)

XPO1-IN-1 (compound D4) (24 h) shows high anti-proliferation efficacy in MM.1S cell and lymphomatous cell lines[1].
XPO1-IN-1 (0-10 μM, 24 h) induces cancer cell cycle arrest[1].
XPO1-IN-1 (0-10 μM, 48 h) induces apoptosis of MM.1S cell[1].
XPO1-IN-1 (0-10 μM, 2 h) inhibits XPO1-dependent nuclear export[1].
XPO1-IN-1 shows the good metabolic stability, with more than 80% intact compound remained over rat plasma (2 h), and around 85% intact compound remained in liver microsomes (1 h)[1].

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

XPO1-IN-1 相关抗体:

Cell Proliferation Assay

Cell Line: MM.1S, Mino, VAL, Rael, Namaiwa, Mutu, H9, JB6, and YT[1]
Concentration:
Incubation Time: 24 h
Result: Showed high anti-proliferation efficacy in MM.1S cell and lymphomatous cell lines (Mino, VAL, Rael, Namaiwa, Mutu, H9, JB6, and YT), with IC50 values of 24, 80.2, 189.1, 201.8, 77.7, 158.2, 101.1, 154.1, and 75.4 nM, respectively.

Cell Cycle Analysis

Cell Line: MM.1S cell[1]
Concentration: 0, 0.1, 1, 5, and 10 μM
Incubation Time: 24 h
Result: Induced cancer cell cycle arrest in high concentration (>100 nM), increased the population of cells arrested in G2 to 37.3% in 5 μM.

Apoptosis Analysis

Cell Line: MM.1S cell[1]
Concentration: 0, 0.1, 1, and 10 μM
Incubation Time: 48 h
Result: Induced apoptosis, significantly increased the apoptotic cell rate to 64.7% (10 μM) when compared to the sample with negative control (6.7%).

Immunofluorescence

Cell Line: MM.1S cell[1]
Concentration: 0, 0.1, 1, and 10 μM
Incubation Time: 2 h
Result: Inhibited XPO1-dependent nuclear export.
体内研究
(In Vivo)

XPO1-IN-1 (compound D4) (Sprague Dawley rats; 10 mg/kg, IG; 1 mg/kg, IV; once) shows a good pharmacokinetic properties[1]. Pharmacokinetic Parameters of XPO1-IN-1 in SD rats[1].

Parameters i.g. (10 mg/kg) i.v. (1 mg/kg)
Tmax (h) 2.17 ± 1.76 0.08
T1/2 (h) 2.12 ± 0.16 2.32 ± 0.17
Cmax (ng/mL) 1391.27 ± 586.77 1239.08 ± 152.54
AUC0-t (ng/mL·h) 5774.13 ± 1461.41 1668.03 ± 229.48
AUC0-∞ (ng/mL·h) 6387.17 ± 1637.18 1791.40 ± 236.56
CL (mL/h/kg) 1638.65 ± 431.97 565.30 ± 80.40
F (%) 34.6

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

Animal Model: Sprague Dawley rats[1]
Dosage: 10 mg/kg (IG), 1 mg/kg (IV)
Administration: Oral gavage (IG), IV, once (Pharmacokinetic Analysis)
Result: Showed a good pharmacokinetic properties, with relatively long half-life of 2.12 h (IG) and 2.32 h (IV), respectively, and decent bioavailability F (%) of 34.6%.
分子量

519.42

Formula

C20H15F6N5O3S
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

XPO1-IN-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:

XPO1-IN-1ApoptosisMultiple myeloma (MM)MM.1S cellLymphomaOrally activeInhibitorinhibitorinhibit

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：
XPO1-IN-1
目录号：
HY-144763
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