Tyrphostin AG 1296

Modify Date: 2024-01-04 09:53:27

Tyrphostin AG 1296 structure	Common Name	Tyrphostin AG 1296
	CAS Number	146535-11-7	Molecular Weight	266.295
	Density	1.2±0.1 g/cm3	Boiling Point	420.2±40.0 °C at 760 mmHg
	Molecular Formula	C₁₆H₁₄N₂O₂	Melting Point	N/A
	MSDS	N/A	Flash Point	151.8±17.6 °C

Use of Tyrphostin AG 1296

Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range[1][2][3].

Name	6,7-dimethoxy-2-phenylquinoxaline
Synonym	More Synonyms

Description	Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range[1][2][3].
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Research Areas >> Cardiovascular Disease Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PDGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3 Research Areas >> Inflammation/Immunology Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit
Target	PDGFRα PDGFRβ
In Vitro	Tyrphostin AG1296 (0.625-20 μM; 72 h) suppresses viability of PLX4032-resistant melanoma cells[4]. Tyrphostin AG1296 (2.5-20 μM; 48 h) induces apoptosis of A375R cells[4]. Tyrphostin AG1296 (5 and 20 μM; 2 h) inhibits PDGFR phosphorylation in A375R cells[4]. Tyrphostin AG1296 (0.0625-1 μM; 8 h) inhibits migration of A375R cells[4]. Cell Viability Assay[4] Cell Line: PLX4032-resistant cell lines (A375R and SK-MEL-5R) Concentration: 0.625, 1.25, 5, 20 μM Incubation Time: 72 h Result: Reduced the viability of both PLX4032-sensitive and PLX4032-resistant cell lines. Apoptosis Analysis[4] Cell Line: A375R cells Concentration: 2.5, 5, 10, 20 μM Incubation Time: 48 h Result: Induced dramatic apoptosis in A375R cells. Western Blot Analysis[4] Cell Line: A375R cells Concentration: 5, 20 μM Incubation Time: 2 h Result: Inhibited phosphorylation of both PDGFR-α and PDGFR-β.
In Vivo	Tyrphostin AG1296 (40 and 80 mg/kg; i.p. daily for two weeks) suppresses A375R tumor growth in vivo[4]. Tyrphostin AG1296 (2 mg/kg; i.p. every other day for 3 weeks) inhibits the atherosclerotic plaque progression and enhances plaque stability by inhibiting inflammatory responses, reducing the expression of matrix metalloproteinases and promoting macrophages from proinflammatory phenotype to anti-inflammatory phenotype[5]. Animal Model: Nud/nud mice are injected with A375R cells[4] Dosage: 40, 80 mg/kg Administration: I.p. daily for two weeks Result: Led to an intermediate level of tumor growth suppression at dose of 40 mg/kg, and significant inhibition of A375R tumor growth at dose of 80 mg/kg. Well tolerated by healthy mice without significant signs of overt toxicity or weight loss.
References	[1]. Gazit A, etm, al. Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole tyrphostins. Comparative Study J Med Chem. 1996 May 24; 39(11): 2170-7. [2]. Kovalenko M, et, al. Selective platelet-derived growth factor receptor kinase blockers reverse sis-transformation. Cancer Res. 1994 Dec 1; 54(23): 6106-14. [3]. Tse KF, et, al. Inhibition of the transforming activity of FLT3 internal tandem duplication mutants from AML patients by a tyrosine kinase inhibitor. Leukemia. 2002 Oct; 16(10): 2027-36. [4]. Li Y, et, al. Tyrphostin AG1296, a platelet-derived growth factor receptor inhibitor, induces apoptosis, and reduces viability and migration of PLX4032-resistant melanoma cells. Onco Targets Ther. 2015 May 14; 8: 1043-51. [5]. Dong M, et, al. AG1296 enhances plaque stability via inhibiting inflammatory responses and decreasing MMP-2 and MMP-9 expression in ApoE-/- mice. Biochem Biophys Res Commun. 2017 Aug 5;489(4):426-431.

Density	1.2±0.1 g/cm3
Boiling Point	420.2±40.0 °C at 760 mmHg
Molecular Formula	C₁₆H₁₄N₂O₂
Molecular Weight	266.295
Flash Point	151.8±17.6 °C
Exact Mass	266.105530
PSA	44.24000
LogP	3.76
Vapour Pressure	0.0±1.0 mmHg at 25°C
Index of Refraction	1.618
Storage condition	2-8°C

Tyrphostin AG 1296 MSDS(Chinese)

WGK Germany	3

1,2-DIMETHOXY-4...

CAS#:3395-03-7

Tyrphostin AG 1296

CAS#:146535-11-7

Literature: Gazit, Aviv; App, Harald; McMahon, Gerald; Chen, Jefferey; Levitzki, Alexander; Bohmer, Frank D. Journal of Medicinal Chemistry, 1996 , vol. 39, # 11 p. 2170 - 2177

Phenylglyoxal

CAS#:1074-12-0

1,2-Diamino-4,5...

CAS#:27841-33-4

Tyrphostin AG 1296

CAS#:146535-11-7

Literature: Gazit, Aviv; App, Harald; McMahon, Gerald; Chen, Jefferey; Levitzki, Alexander; Bohmer, Frank D. Journal of Medicinal Chemistry, 1996 , vol. 39, # 11 p. 2170 - 2177

Precursor 3
CAS#:3395-03-7 1,2-DIMETHOXY-4... CAS#:1074-12-0 Phenylglyoxal CAS#:27841-33-4 1,2-Diamino-4,5...
DownStream 0

6,7-Dimethoxy-2-phenylquinoxaline

Quinoxaline, 6,7-dimethoxy-2-phenyl-

Quinoxaline,6,7-dimethoxy-2-phenyl

2-phenyl-6,7-dimethoxyquinoxaline

Tyrphostin AG-1296

2-phenyl-6,7-dimetoxyquinoxaline

MFCD00270913

6,7-Dimethoxy-3-phenylquinoxaline

DC Chemicals Limited
China
Product Name: AG-1296
Price: $500.0/100mg $850.0/250mg $1600.0/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: TYRPHOSTIN AG 1296
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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Tyrphostin AG 1296

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