AG-1024 structure
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Common Name | AG-1024 | ||
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| 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-1024AG-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 |
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| 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]. |
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| Related Catalog | |
| References |
| 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 |
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| WGK Germany | 3 |
| HS Code | 2926909090 |
| Precursor 2 | |
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| DownStream 0 | |
| HS Code | 2926909090 |
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| 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 |