2. Protein Tyrosine Kinase/RTK Membrane Transporter/Ion Channel Apoptosis
  3. VEGFR P-glycoprotein Apoptosis
  4. VEGFR-2/P-gp-IN-1

VEGFR-2/P-gp-IN-1 是一种 Licochalcone A (HY-N0372) 衍生物，是一种具口服活性的 VEGFR-2 (IC50 = 0.885 μM) 和 P-糖蛋白 (P-gp) 抑制剂。 VEGFR-2/P-gp-IN-1 通过同步抑制 VEGFR-2 激酶活性和 P-gp 药物外排泵功能，实现抗肿瘤增殖并克服化疗耐药性。VEGFR-2/P-gp-IN-1 可抑制 VEGFR-2 以及下游PI3K/AKT 信号通路蛋白的磷酸化，诱导细胞凋亡 (Apoptosis)，将细胞阻滞在 S 期，并抑制侵袭性迁移。VEGFR-2/P-gp-IN-1 在 HeLa/DDP 细胞异种移植瘤模型中展现出强大的体内抗肿瘤作用。VEGFR-2/P-gp-IN-1 可用于宫颈癌的研究。

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

VEGFR-2/P-gp-IN-1 Chemical Structure

VEGFR-2/P-gp-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

VEGFR-2/P-gp-IN-1 相关抗体

Top Publications Citing Use of Products

查看 VEGFR 亚型特异性产品:

查看所有亚型
VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VEGFR-2/P-gp-IN-1, a Licochalcone A (HY-N0372) derivative, is an orally active VEGFR-2 (IC50 = 0.885 μM) and P-gp inhibitor. VEGFR-2/P-gp-IN-1 achieves anti-tumor proliferation and overcomes chemotherapy resistance by synchronously inhibiting VEGFR-2 kinase activity and P-gp drug efflux pump function. VEGFR-2/P-gp-IN-1 inhibits phosphorylation of VEGFR-2 and downstream PI3K/AKT signaling pathway proteins, induces apoptosis, blocks cells in the S phase, and inhibits invasive migration. VEGFR-2/P-gp-IN-1 exerts potent in vivo anti-tumor effects in the HeLa/DDP cell xenograft tumor model. VEGFR-2/P-gp-IN-1 is used in cervical cancer research[1].

体外研究
(In Vitro)

VEGFR-2/P-gp-IN-1 (Compound A20) (1-100 μM, 48 h) 显著抑制宫颈癌细胞 (含耐药株) 的增殖[1]。

VEGFR-2/P-gp-IN-1 (1-6 μM, 24 h) 通过双重靶向抑制 VEGFR-2 磷酸化与 P-gp 外排功能，克服宫颈癌耐药性[1]。

VEGFR-2/P-gp-IN-1 (1-4 μM，24 h) 在 HeLa/DDP 细胞系中通过激活细胞凋亡途径杀死癌细胞，在 S 期阻断细胞周期进程以抑制增殖，并显著抑制癌细胞的侵袭和迁移[1]。

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

VEGFR-2/P-gp-IN-1 相关抗体:

Western Blot Analysis[1]

Cell Line: HeLa-DDP cells, HUVEC cells
Concentration: 1 μM, 2 μM, 4 μM, 6μM
Incubation Time: 24 h
Result: Dose-dependently inhibited VEGFR-2 and downstream PI3K/AKT phosphorylation.
Upregulated the pro-apoptotic protein Bax, downregulated the anti-apoptotic protein Bcl-2, and did not alter the expression level of P-gp protein.

Cell Viability Assay[1]

Cell Line: HeLa/DDP drugresistant cells, HeLa/PTX drugresistant cells, HeLa/ADR drugresistant cells
Concentration: 1.0 μM, 6.25 μM, 12.5 μM, 25 μM, 50 μM, 100 μM
Incubation Time: 48 h
Result: Showed the most significant inhibitory activity against these three drug-resistant cervical cancer cell lines, with IC50 values of 3.69 μM (HeLa/DDP), 4.81 μM (HeLa/PTX), and 5.98 μM (HeLa/ADR), compared with HeLa cells, the resistance indices (RIs) were 1.16, 1.51, and 1.87, respectively.

Apoptosis Analysis[1]

Cell Line: HeLa/DDP cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Induced apoptosis in HeLa cells at a rate of 92.3% at a concentration of 4 μM.
Induced apoptosis in HeLa/DDP cells at a rate of 94.5% at a concentration of 4 μM.

Cell Cycle Analysis[1]

Cell Line: HeLa/DDP cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Induced S-phase arrest in HeLa cells at 39.32% at a concentration of 4 μM.
Induced S-phase arrest in HeLa/DDP cells at 39.04% at a concentration of 4 μM.

Immunofluorescence[1]

Cell Line: HeLa/DDP cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Reduced the fluorescence intensity of p-VEGFR-2 in HeLa/HeLa-DDP cells in a dose-dependent manner.

Cell Invasion Assay[1]

Cell Line: HeLa/DDP cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Reduced invasive potential of HeLa/DDP cells to 209, 142, and 54 cells at concentrations of 1, 2, and 4 μM.
Reduced invasive potential of HeLa cells to 360, 219, and 106 cells at concentrations of 1, 2, and 4 μM.

Cell Migration Assay [1]

Cell Line: HeLa/DDP cells
Concentration: 1 μM, 2 μM, 4 μM
Incubation Time: 24 h
Result: Reduced penetration capacity of HeLa/DDP cells into the ventricular membrane to 268, 178, and 85 cells at concentrations of 1, 2, and 4 μM, respectively.
Reduced penetration capacity of HeLa cells through the ventricular membrane to 583, 286, and 226 cells at concentrations of 1, 2, and 4 μM.
体内研究
(In Vivo)

VEGFR-2/P-gp-IN-1 (Compound A20) (10 mg/kg, 20 mg/kg, 40 mg/kg, i.g., 每日一次, 持续 14 天) 在 HeLa/DDP 细胞异种移植小鼠模型中显示出治疗顺铂耐药性宫颈癌的潜力，且安全性良好，未表现显著毒性[1]。

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

Animal Model: HeLa/DDP cell xenograft model established in BALB/C nude female mice (4-5 weeks)[1]
Dosage: 10 mg/kg, 20 mg/kg, 40 mg/kg
Administration: Daily intragastric gavage (i.g.), at the corresponding doses for 14 days.
Result: Suppressed grafted tumors by 70.9%, 72.2%, and 89.5% at doses of 10, 20, and 40 mg/kg (positive control sorafenib 20 mg/kg: 36.1% reduction).
Inhibited growth of drug-resistant cervical cancer xenografts dose-dependently via oral administration.
Maintained comparable body weight across all groups.
Animal Model: Female Kunming mice (5 weeks, 20-22 g)[1]
Dosage: 200 mg/kg
Administration: Daily intragastric gavage (i.g.), at the corresponding doses for 14 days.
Result: Caused no mortality or significant body weight changes versus controls in acute mouse toxicity testing.
Induced normal liver/kidney function without necrosis, structural disorder, or inflammatory infiltration in acute mouse toxicity testing.
Demonstrated safety at 200 mg/kg without significant toxicity.
分子量

502.45

Formula

C24H24F6N2O3
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

VEGFR-2/P-gp-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:

VEGFR-2/P-gp-IN-1VEGFRP-glycoproteinApoptosisVascular endothelial growth factor receptorP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243VEGFR-2Cisplatin-resistant cervical cancerHeLa cellsBALB/C nude miceInhibitorinhibitorinhibit

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：
VEGFR-2/P-gp-IN-1
目录号：
HY-174324
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