製品番号: HY-109019

Vorolanib

(別名: CM082; X-82)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).

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純度: 99.78%
CAS 番号: 1013920-15-4
分子式: C₂₃H₂₆FN₅O₃
分子量:439.48

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Vorolanib 構造式

CAS 番号: 1013920-15-4

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- Cellular Effect
- 体外実験
- 体内実験
- 臨床実験
化学情報
Publications (1)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
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生物活性

製品説明

VEGFR アイソフォーム固有の製品をすべて表示 :

PDGFR アイソフォーム固有の製品をすべて表示 :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	0.0155 μM Compound: CM082	Cytotoxicity against HEK293 cells expressing ABCG2-R-482 wildtype assessed as decrease in mitoxantrone half inhibitory concentration Cytotoxicity against HEK293 cells expressing ABCG2-R-482 wildtype assessed as decrease in mitoxantrone half inhibitory concentration	[PMID: 35944339]
HEK293	IC₅₀	0.058 μM Compound: CM082	Cytotoxicity against HEK293 cells expressing ABCG2-R-482 mutant assessed as decrease in mitoxantrone half inhibitory concentration Cytotoxicity against HEK293 cells expressing ABCG2-R-482 mutant assessed as decrease in mitoxantrone half inhibitory concentration	[PMID: 35944339]
HUVEC	IC₅₀	31.5 nM Compound: CM082; X-82	Inhibition of VEGF-induced HUVECs proliferation Inhibition of VEGF-induced HUVECs proliferation	[PMID: 37285684]

体外実験

Vorolanib (CM082; 1-100 μM) can specifically enhance the sensitivity of a substrate chemotherapeutical agent in overexpressing ABCG2 cells, but not in overexpressing ABCB1 cells. Vorolanib (1.25, 2.5, 5.0, 20 μM) does not influence the expression of ABCG2 in mRNA or protein Levels^[1].
? Vorolanib (0.001-10 μM) inhibits the growth of VEGF‐stimulated HUVECs (IC₅₀=0.031 μM) and FBS‐stimulated HUVEC growth (IC₅₀=29.9?μM)^[2].
? Vorolanib (0.01, 0.1, 1 μM) exhibits a concentration‐dependent inhibition on VEGF‐induced (40 ng/mL) phosphorylation of VEGFR2 and its downstream signaling molecules ERK1/2, AKT, and STAT3 in HUVECs. Vorolanib (0.1, 1 μM) inhibits FBS‐stimulated tube formation and cell migration of HUVECs in a concentration‐dependent manner^[2].

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

体内実験

Vorolanib (CM082; 20 mg/kg; gavage; once every 2 days; 1 h before SKF 104864A; for 23 days) enhances the anti-tumor effect of SKF 104864A on xenografts of ABCG2-overexpressing cells^[1].
? Vorolanib (80 mg/kg; twice daily; for 21 days) has antitumor activity combined with ZD1839 (10 mg/kg; q.d; for 21 days) on H3255 tumor xenograft (female BALB/c nude mice aged five weeks)^[2].

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

臨床実験

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

化学情報

CAS 番号 1013920-15-4
性状 Solid
分子量 439.48
分子式 C₂₃H₂₆FN₅O₃
Color Light yellow to yellow
SMILES

O=C1/C(C2=CC(F)=CC=C2N1)=C/C(NC(C)=C3C(N[C@@H]4CN(C(N(C)C)=O)CC4)=O)=C3C
別名

CM082; X-82
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (1)

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Journal Impact Factor

bioRxiv

2026 Apr 21.

溶剤 & 溶解度

体外:

DMSO : 27 mg/mL (61.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2754 mL

11.3771 mL

22.7542 mL

5 mM

0.4551 mL

2.2754 mL

4.5508 mL

10 mM

0.2275 mL

1.1377 mL

2.2754 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.25 mg/mL (5.12 mM); Clear solution

This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (272 KB)
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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
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MS (2659 KB)
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OR (2659 KB)
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SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Lejia Xu, et al. CM082 Enhances the Efficacy of Chemotherapeutic Drugs by Inhibiting the Drug Efflux Function of ABCG2. Mol Ther Oncolytics. 2019 Dec 27;16:100-110. [Content Brief]

[2]. Kun Zhang, et al. CM082, a novel angiogenesis inhibitor, enhances the antitumor activity of ZD1839 on epidermal growth factor receptor mutant non-small cell lung cancer in vitro and in vivo. Thorac Cancer. 2020 Jun;11(6):1566-1577. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2754 mL	11.3771 mL	22.7542 mL	56.8854 mL
	5 mM	0.4551 mL	2.2754 mL	4.5508 mL	11.3771 mL
	10 mM	0.2275 mL	1.1377 mL	2.2754 mL	5.6885 mL
	15 mM	0.1517 mL	0.7585 mL	1.5169 mL	3.7924 mL
	20 mM	0.1138 mL	0.5689 mL	1.1377 mL	2.8443 mL
	25 mM	0.0910 mL	0.4551 mL	0.9102 mL	2.2754 mL
	30 mM	0.0758 mL	0.3792 mL	0.7585 mL	1.8962 mL
	40 mM	0.0569 mL	0.2844 mL	0.5689 mL	1.4221 mL
	50 mM	0.0455 mL	0.2275 mL	0.4551 mL	1.1377 mL
	60 mM	0.0379 mL	0.1896 mL	0.3792 mL	0.9481 mL

Vorolanib

1 Cited Publications

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Vorolanib

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MedChemExpress（MCE）の使用を引用している文献 Vorolanib

VEGFR アイソフォーム固有の製品をすべて表示

PDGFR アイソフォーム固有の製品をすべて表示

生物活性

化学情報

Publications (1)

溶剤 & 溶解度

純度とドキュメンテーション

参考文献

Help & FAQs

Complete Stock Solution Preparation Table

Vorolanib 関連分類

HY-109019 関連分類