製品番号: HY-13737

R1530

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

R1530 is a highly potent, orally active, dual-acting mitosis/angiogenesis inhibitor, with anti-tumor and anti-angiogenic activities. R1530 is a multikinase inhibitor which binds to 31 kinases with K_d values of <500 nM. R1530 inhibits VGFR2 and FGFR1 with IC₅₀ of 10 nM and 28 nM, respectively. R1530 triggers apoptosis (mitotic catastrophe) or senescence.

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研究用途以外に使用した場合、当社は一切の責任を負いかねます。

純度: 98.29%
CAS 番号: 882531-87-5
分子式: C₁₈H₁₄ClFN₄O
分子量:356.78

保管条件:

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

R1530 構造式

CAS 番号: 882531-87-5

容量

価格（税別）

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数量

Amount: USD 0.00

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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
- IC₅₀ & Target
- Cellular Effect
- 体外実験
- 体内実験
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
Bioz

生物活性

製品説明

IC₅₀ & Target^[1]

KDR

10 nM (IC₅₀)

FGFR1

28 nM (IC₅₀)

VEGFR 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
Cancer cell lines	IC₅₀	0.2 μM Compound: 2, R1530	Antiproliferative activity against human breast cancer cells by MTT assay Antiproliferative activity against human breast cancer cells by MTT assay	[PMID: 24900658]
Cancer cell lines	IC₅₀	0.2 μM Compound: 2, R1530	Antiproliferative activity against human colon cancer cells by MTT assay Antiproliferative activity against human colon cancer cells by MTT assay	[PMID: 24900658]
Cancer cell lines	IC₅₀	0.2 μM Compound: 2, R1530	Antiproliferative activity against human lung cancer cells by MTT assay Antiproliferative activity against human lung cancer cells by MTT assay	[PMID: 24900658]
Cancer cell lines	IC₅₀	0.2 μM Compound: 2, R1530	Antiproliferative activity against human oral epidermoid cancer cells by MTT assay Antiproliferative activity against human oral epidermoid cancer cells by MTT assay	[PMID: 24900658]
Cancer cell lines	IC₅₀	0.2 μM Compound: 2, R1530	Antiproliferative activity against human prostate cancer cells by MTT assay Antiproliferative activity against human prostate cancer cells by MTT assay	[PMID: 24900658]
HUVEC	IC₅₀	118 nM Compound: 2, R1530	Antiangiogenic activity in HUVEC assessed as inhibition of bFGF-induced cell proliferation Antiangiogenic activity in HUVEC assessed as inhibition of bFGF-induced cell proliferation	[PMID: 24900658]
HUVEC	IC₅₀	49 nM Compound: 2, R1530	Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced cell proliferation	[PMID: 24900658]
HUVEC	IC₅₀	688 nM Compound: 2, R1530	Antiangiogenic activity in HUVEC assessed as inhibition of PDGF-induced cell proliferation Antiangiogenic activity in HUVEC assessed as inhibition of PDGF-induced cell proliferation	[PMID: 24900658]
Melanoma cell	IC₅₀	0.2 μM Compound: 2, R1530	Antiproliferative activity against human melanoma cells by MTT assay Antiproliferative activity against human melanoma cells by MTT assay	[PMID: 24900658]

体外実験

R1530 exhibits potent in vitro antiproliferative activity in all of the tumor cell lines ( IC₅₀ = 0.2 3.4 μM)^[1].
R1530 inhibits the kinase activities of vascular endothelial growth factor receptor 2 (VGFr2), FGFr1 and PDGFr-β. R1530 has inhibition of VEGF and bFGF induces HUVEC proliferation ( IC₅₀ = 49 and 118 nM)^[1].

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

体内実験

R1530 (1.56, 25, and 50 mg/kg; p.o.; daily, for 28 days.) has notable antitumor activity across a broad range of human xenograft models, with minimal toxicity^[1].

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

Animal Model:

Human tumor xenograft models^[1]
Dosage:

1.56, 25 and 50 mg/kg
Administration:

Oral administration; daily, for 28 days.
Result:

Inhibited tumor growth in all models, with regression observed in all models tested at a 50 mg/kg dose.

化学情報

CAS 番号 882531-87-5
性状 Solid
分子量 356.78
分子式 C₁₈H₁₄ClFN₄O
Color Light yellow to yellow
SMILES

CC(NN1)=C2C1=NC3=CC(OC)=C(F)C=C3C(C4=CC=CC=C4Cl)=N2
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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Comput Struct Biotechnol J

Unveiling the Kinomes of Leishmania infantum and L. braziliensis Empowers the Discovery of New Kinase Targets and Antileishmanial Compounds. [Abstract]

2019 Feb 8:17:352-361. PMID: 30949306

溶剤 & 溶解度

体外:

DMSO : 50 mg/mL (140.14 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

2.8028 mL

14.0142 mL

28.0285 mL

5 mM

0.5606 mL

2.8028 mL

5.6057 mL

10 mM

0.2803 mL

1.4014 mL

2.8028 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 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.01 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

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 (279 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[1]. Jin-Jun Liu, et al. Discovery of a Highly Potent, Orally Active Mitosis/Angiogenesis Inhibitor R1530 for the Treatment of Solid Tumors. ACS Med Chem Lett. 2013 Feb 14; 4(2): 259–263. [Content Brief]

[2]. Christian Tovar, et al. Small-molecule inducer of cancer cell polyploidy promotes apoptosis or senescence: Implications for therapy. Cell Cycle. 2010 Aug 15;9(16):3364-75. [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	2.8028 mL	14.0142 mL	28.0285 mL	70.0712 mL
	5 mM	0.5606 mL	2.8028 mL	5.6057 mL	14.0142 mL
	10 mM	0.2803 mL	1.4014 mL	2.8028 mL	7.0071 mL
	15 mM	0.1869 mL	0.9343 mL	1.8686 mL	4.6714 mL
	20 mM	0.1401 mL	0.7007 mL	1.4014 mL	3.5036 mL
	25 mM	0.1121 mL	0.5606 mL	1.1211 mL	2.8028 mL
	30 mM	0.0934 mL	0.4671 mL	0.9343 mL	2.3357 mL
	40 mM	0.0701 mL	0.3504 mL	0.7007 mL	1.7518 mL
	50 mM	0.0561 mL	0.2803 mL	0.5606 mL	1.4014 mL
	60 mM	0.0467 mL	0.2336 mL	0.4671 mL	1.1679 mL
	80 mM	0.0350 mL	0.1752 mL	0.3504 mL	0.8759 mL
	100 mM	0.0280 mL	0.1401 mL	0.2803 mL	0.7007 mL

Keywords

R1530

1 Cited Publications

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R1530

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Obesity Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Anti-Prostate Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cytokine Inhibitors Library

Cell Death Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Fibrosis Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

MedChemExpress（MCE）の使用を引用している文献 R1530

VEGFR 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

R1530 関連分類

HY-13737 関連分類