R1530

Name: R1530
Brand: MedChemExpress
SKU: HY-13737
Rating: 4.5 (1 reviews)

Cat. No.: HY-13737 Purity: 98.29%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

For research use only. We do not sell to patients.

R1530 Chemical Structure

CAS No. : 882531-87-5

Size	Price	Stock	Quantity
Free Sample (0.1 - 0.5 mg)		Apply Now
5 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 170	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 355	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 568	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 860	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE R1530

•Comput Struct Biotechnol J. 2019 Feb 8;17:352-361. [Abstract]

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

KDR

10 nM (IC₅₀)

FGFR1

28 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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 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]
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.

Molecular Weight

356.78

Formula

C₁₈H₁₄ClFN₄O

CAS No.

882531-87-5

Appearance

Solid

Color

Light yellow to yellow

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.06%

Select Batch:

Data Sheet (280 KB) SDS (393 KB)

COA (257 KB) LCMS (124 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

R1530 Related Classifications

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:

R1530882531-87-5R 1530R-1530VEGFRFGFRApoptosisVascular endothelial growth factor receptorFibroblast growth factor receptormitoticmitosisangiogenesisantitumorantiproliferativeInhibitorinhibitorinhibit

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R1530

Customer Review

R1530 Related Antibodies

1 Publications Citing Use of MCE R1530

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All VEGFR Isoform Specific Products:

View All FGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

R1530 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

R1530 Related Classifications

Keywords:

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