AG 1295

Name: AG 1295
Brand: MedChemExpress
SKU: HY-101957
Rating: 5.0 (3 reviews)

Cat. No.: HY-101957 Purity: 99.90%: FAQs
Data Sheet SDS COA Handling Instructions

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AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor.

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

AG 1295 Chemical Structure

CAS No. : 71897-07-9

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 66	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 66	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 60	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 100	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 300	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 3 publication(s) in Google Scholar

3 Publications Citing Use of MCE AG 1295

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PDGFR PDGFRβ PDGFRα

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

PDGFR^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
MV4-11	IC₅₀	2.2 μM Compound: AG1295	Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay	[PMID: 32659083]
NIH3T3	IC₅₀	0 μM Compound: AG-1295	Antitumor activity measured by the inhibition of platelet-derived growth factor receptor autophosphorylation in intact Swiss 3T3 cells Antitumor activity measured by the inhibition of platelet-derived growth factor receptor autophosphorylation in intact Swiss 3T3 cells	[PMID: 11855980]
SF-539	IC₅₀	6.2 μM Compound: 28	Inhibition of PDGF-BB-induced PDGFR beta phosphorylation in human SF539 cells overexpressing PDGFR beta pretreated for 60 mins prior to PDGF-BB addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis Inhibition of PDGF-BB-induced PDGFR beta phosphorylation in human SF539 cells overexpressing PDGFR beta pretreated for 60 mins prior to PDGF-BB addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis	[PMID: 23375090]
SF-539	IC₅₀	6.2 μM Compound: 22, AG-1295	Inhibition of PDGFBB-induced PDGFRbeta autophosphorylation in human SF539 cells incubated for 60 mins prior to PDGFBB-induction measured after 10 mins by phosphotyrosine ELISA Inhibition of PDGFBB-induced PDGFRbeta autophosphorylation in human SF539 cells incubated for 60 mins prior to PDGFBB-induction measured after 10 mins by phosphotyrosine ELISA	[PMID: 22370340]
U-251	IC₅₀	6.2 μM Compound: 18, AG-1295	Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA	[PMID: 19748785]

In Vitro

AG 1295 inhibits PDGFR autophosphorylation with IC₅₀s of 0.3-0.5 μM and 0.5-1 μM for membrane autophosphorylation assays and Swiss 3T3 cells, respectively^[1].
AG1295 (10 μM, 100 μM) significantly inhibits rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB in vitro^[2].

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

Cell Viability Assay^[2]

Cell Line:	Rabbit conjunctival fibroblasts cells
Concentration:	1 μM, 10 μM, 100 μM
Incubation Time:	3 days
Result:	Inhibited rabbit conjunctival fibroblast cell growth stimulated by PDGF-AA or PDGF-BB.

In Vivo

AG-1295 reduces neointimal formation in aortic allograft vasculopathy by inhibition of PDGFR-beta-triggered tyrosine phosphorylation^[3].
AG1295 (12 mg/kg; i.p.; daily; for 14 or 21 days) significantly reduces interstitial fibrosis as verified by a smaller Sirius-Red stained area and also by a reduced number of macrophages, and by the ED-A+ fibronectin deposition and the number of cells positive for alpha-smooth muscle actin^[4].

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

Animal Model:	Sprague-Dawley rats (240-270 g)^[4]
Dosage:	12 mg/kg
Administration:	Intraperitoneal injection; daily; for 14 or 21 days
Result:	Attenuated interstitial fibrosis in rat kidney after unilateral obstruction.

Molecular Weight

234.30

Formula

C₁₆H₁₄N₂

CAS No.

71897-07-9

Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=C(C)C=C2N=CC(C3=CC=CC=C3)=NC2=C1

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 (213.40 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	4.2680 mL	21.3402 mL	42.6803 mL
5 mM	0.8536 mL	4.2680 mL	8.5361 mL
10 mM	0.4268 mL	2.1340 mL	4.2680 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.

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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 Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

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

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.90%

Select Batch:

Data Sheet (276 KB) SDS (251 KB)

COA (248 KB) LCMS (304 KB)

Handling Instructions (2659 KB)

References

[1]. Kovalenko M, et al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Res. 1994 Dec 1;54(23):6106-14. [Content Brief]

[2]. Zheng Y, et al. Platelet-derived growth factor receptor kinase inhibitor AG1295 and inhibition of experimental proliferative vitreoretinopathy. Jpn J Ophthalmol. 2003 Mar-Apr;47(2):158-65. [Content Brief]

[3]. Inhibition of aortic allograft vasculopathy by local delivery of platelet-derived growth factor receptor tyrosine-kinase blocker AG-1295. Transplantation. 2002 Nov 15;74(9):1335-41. [Content Brief]

[4]. Ludewig D, et al. PDGF receptor kinase blocker AG1295 attenuates interstitial fibrosis in rat kidney after unilateral obstruction. Cell Tissue Res. 2000 Jan;299(1):97-103. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	4.2680 mL	21.3402 mL	42.6803 mL	106.7008 mL
	5 mM	0.8536 mL	4.2680 mL	8.5361 mL	21.3402 mL
	10 mM	0.4268 mL	2.1340 mL	4.2680 mL	10.6701 mL
	15 mM	0.2845 mL	1.4227 mL	2.8454 mL	7.1134 mL
	20 mM	0.2134 mL	1.0670 mL	2.1340 mL	5.3350 mL
	25 mM	0.1707 mL	0.8536 mL	1.7072 mL	4.2680 mL
	30 mM	0.1423 mL	0.7113 mL	1.4227 mL	3.5567 mL
	40 mM	0.1067 mL	0.5335 mL	1.0670 mL	2.6675 mL
	50 mM	0.0854 mL	0.4268 mL	0.8536 mL	2.1340 mL
	60 mM	0.0711 mL	0.3557 mL	0.7113 mL	1.7783 mL
	80 mM	0.0534 mL	0.2668 mL	0.5335 mL	1.3338 mL
	100 mM	0.0427 mL	0.2134 mL	0.4268 mL	1.0670 mL

AG 1295 Related Classifications

Cardiovascular Disease

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:

AG 129571897-07-9AG1295AG-1295PDGFRPlatelet-derived growth factor receptorRTKPDGF-receptorautophosphorylationInhibitorinhibitorinhibit

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AG 1295

Customer Review

AG 1295 Related Antibodies

3 Publications Citing Use of MCE AG 1295

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All PDGFR Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

AG 1295 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AG 1295 Related Classifications

Keywords:

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