AG-1024

Modify Date: 2024-01-08 23:49:19

AG-1024 structure	Common Name	AG-1024
	CAS Number	65678-07-1	Molecular Weight	305.170
	Density	1.4±0.1 g/cm3	Boiling Point	379.8±42.0 °C at 760 mmHg
	Molecular Formula	C₁₄H₁₃BrN₂O	Melting Point	N/A
	MSDS	N/A	Flash Point	183.5±27.9 °C

Use of AG-1024

AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, less potent to IR with IC50 of 57 μM.IC50 value: 7 uM (IGF-1R autophosphorylation); 57 uM (IR) [1]Target: IGF-1R; IRin vitro: AG-1024 blocks the IGF-1 receptor and IR autophosphorylation with IC50 of 7 μM and 57 μM, respectively. AG-1024 also inhibits the receptor tyrosine kinase activity towards exogenous substrates (TKA) with IC50 values of 18 μM and 80 μM, respectively [1]. Human breast cancer cell line MCF-7 exposure to Tyrphostin AG 1024 inhibited proliferation and induced apoptosis in a time-dependent manner, and the degree of growth inhibition for IC20 plus irradiation (4 Gy) was up to 50% compared to the control. Examination of Tyrphostin AG 1024 effects on radiation response demonstrated a marked enhancement in radiosensitivity and amplification of radiation-induced apoptosis [2]. AG-1024 significantly inhibits melanoma cell proliferation with an IC50 of <50 nM in the absence of serum, by blocking MAPK/ERK2 signaling, subsequently rapidly inducing pRb dephosphorylation and activation, and eventually the formation of growth suppressive pRb-E2F complexes [3].in vivo: Administration of AG-1024 at a dose of 30 μg for 10 days significantly inhibits the tumor growth of Ba/F3-p210 xenograft in mice [4].

Name	2-[(3-bromo-5-tert-butyl-4-hydroxyphenyl)methylidene]propanedinitrile
Synonym	More Synonyms

Description	AG-1024 (Tyrphostin) inhibits IGF-1R autophosphorylation with IC50 of 7 μM, less potent to IR with IC50 of 57 μM.IC50 value: 7 uM (IGF-1R autophosphorylation); 57 uM (IR) [1]Target: IGF-1R; IRin vitro: AG-1024 blocks the IGF-1 receptor and IR autophosphorylation with IC50 of 7 μM and 57 μM, respectively. AG-1024 also inhibits the receptor tyrosine kinase activity towards exogenous substrates (TKA) with IC50 values of 18 μM and 80 μM, respectively [1]. Human breast cancer cell line MCF-7 exposure to Tyrphostin AG 1024 inhibited proliferation and induced apoptosis in a time-dependent manner, and the degree of growth inhibition for IC20 plus irradiation (4 Gy) was up to 50% compared to the control. Examination of Tyrphostin AG 1024 effects on radiation response demonstrated a marked enhancement in radiosensitivity and amplification of radiation-induced apoptosis [2]. AG-1024 significantly inhibits melanoma cell proliferation with an IC50 of <50 nM in the absence of serum, by blocking MAPK/ERK2 signaling, subsequently rapidly inducing pRb dephosphorylation and activation, and eventually the formation of growth suppressive pRb-E2F complexes [3].in vivo: Administration of AG-1024 at a dose of 30 μg for 10 days significantly inhibits the tumor growth of Ba/F3-p210 xenograft in mice [4].
Related Catalog	Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IGF-1R Research Areas >> Cancer
References	[1]. Párrizas M, et al. Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997 Apr;138(4):1427-33. [2]. Wen B, et al. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells. Br J Cancer. 2001 Dec 14;85(12):2017-21. [3]. von Willebrand M, et al. The tyrphostin AG1024 accelerates the degradation of phosphorylated forms of retinoblastoma protein (pRb) and restores pRb tumor suppressive function in melanoma cells. Cancer Res. 2003 Mar 15;63(6):1420-9. [4]. Deutsch E, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation. Br J Cancer. 2004 Nov 1;91(9):1735-41.

Description

Related Catalog

Signaling Pathways >> Autophagy >> Autophagy

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> IGF-1R

Research Areas >> Cancer

References

[1]. Párrizas M, et al. Specific inhibition of insulin-like growth factor-1 and insulin receptor tyrosine kinase activity and biological function by tyrphostins. Endocrinology. 1997 Apr;138(4):1427-33.

[2]. Wen B, et al. Tyrphostin AG 1024 modulates radiosensitivity in human breast cancer cells. Br J Cancer. 2001 Dec 14;85(12):2017-21.

[3]. von Willebrand M, et al. The tyrphostin AG1024 accelerates the degradation of phosphorylated forms of retinoblastoma protein (pRb) and restores pRb tumor suppressive function in melanoma cells. Cancer Res. 2003 Mar 15;63(6):1420-9.

[4]. Deutsch E, et al. Tyrosine kinase inhibitor AG1024 exerts antileukaemic effects on STI571-resistant Bcr-Abl expressing cells and decreases AKT phosphorylation. Br J Cancer. 2004 Nov 1;91(9):1735-41.

Density	1.4±0.1 g/cm3
Boiling Point	379.8±42.0 °C at 760 mmHg
Molecular Formula	C₁₄H₁₃BrN₂O
Molecular Weight	305.170
Flash Point	183.5±27.9 °C
Exact Mass	304.021118
PSA	67.81000
LogP	4.18
Appearance of Characters	solid \| yellow
Vapour Pressure	0.0±0.9 mmHg at 25°C
Index of Refraction	1.609
Storage condition	−20°C
Water Solubility	DMSO: soluble

Safety Phrases	22-24/25
WGK Germany	3
HS Code	2926909090

Precursor 2
CAS#:65678-06-0 3-Bromo-5-(tert... CAS#:109-77-3 Malononitrile
DownStream 0

HS Code	2926909090
Summary	HS:2926909090 other nitrile-function compounds VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:30.0%

(3-bromo-5-tert-butyl-4-hydroxybenzylidene)malononitrile

3-bromo-5-t-butyl-4-hydroxy-benzylidene-malononitrile

propanedinitrile, [[3-bromo-5-(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]-

3-Bromo-5-t-butyl-4-hydroxy-benzylidenemalonitrile

2-(3-bromo-5-tert-butyl-4-hydroxybenzylidene)malononitrile

[3-Bromo-4-hydroxy-5-(2-methyl-2-propanyl)benzylidene]malononitrile

2-[(3-bromo-4-hydroxy-5-tert-butyl-phenyl)methylidene]propanedinitrile

Propanedinitrile, 2-[[3-bromo-5-(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]-

Tyrphostin AG 1024

ag1024

propanedinitrile,[[3-bromo-5-(1,1-dimethylethyl)-4-hydroxyphenyl]methylene]

AG-1024

DC Chemicals Limited
China
Product Name: AG-1024 (Tyrphostin)
Price: $1200.0/1g $350.0/100mg $600.0/250mg
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: AG1024
Price: $Inquiry/100g $Inquiry/1kg $Inquiry/100kg $Inquiry/1000kg
Purity: 98.0%
Stocking Period: Inquiry
Contact: Ms Wang

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Price: $90/10mM*1mLinDMSO

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AG-1024

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