Art. -Nr.: HY-13737

R1530

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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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Reinheit: 98.29%
CAS. Nr.: 882531-87-5
Formel: C₁₈H₁₄ClFN₄O
Molecular Weight:356.78

Speicherung:

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

R1530 Chemical Structure

CAS. Nr.: 882531-87-5

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Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

KDR

10 nM (IC₅₀)

FGFR1

28 nM (IC₅₀)

Alle VEGFR Isoform-spezifische Produkte anzeigen :

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]

In Vitro

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.

In Vivo

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.

Chemical Information

CAS. Nr. 882531-87-5
Appearance Solid
Molecular Weight 356.78
Formel C₁₈H₁₄ClFN₄O
Color Light yellow to yellow
SMILES

CC(NN1)=C2C1=NC3=CC(OC)=C(F)C=C3C(C4=CC=CC=C4Cl)=N2
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
Elemental Analysis Report (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)
Handling Instructions (2659 KB)

Verweise

[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

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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

Publications Citing Use of MedChemExpress (MCE) R1530

Alle VEGFR Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

R1530 Related Classifications

HY-13737 Related Classifications