AG-1517, CAS NO.153436-54-5
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- Min.Order: 100 Gram
- Payment Terms: L/C
- Available Specifications:
≥98.0%(100-500)Gram≥98.0%(1000-5000)Gram
- Product Details
Keywords
- AG-1517,
- 4-[(3-BROMOPHENYL)AMINO]-6,7-DIMETHOXYQUINAZOLINE HYDROCHLORIDE;PD 153035 HYDROCHLORIDE;PD153035HCl;4-(3-Bromphenylamino)-6,7-bis(methoxy)quinazoline;4-(3-Bromphenylamino)-6,7-dimethylquinazoline;4-Qu
- 153436-54-5
Quick Details
- ProName: AG-1517,
- CasNo: 153436-54-5
- Molecular Formula: C16H15BrClN3O2
- Appearance: White crystal
- Application: CAS:153436-54-5; Signal transduction ...
- DeliveryTime: 2 months
- PackAge: 100g,500g,1kg,25kg/drum
- Port: shang hai
- ProductionCapacity: 1000 Gram/Week
- Purity: 98%
- Storage: Dry seal
- Transportation: shipping
- LimitNum: 100 Gram
Superiority
Details
PD153035(ZM 252868; AG 1517) is a potent and specific inhibitor of EGFR with Ki and IC50 of 5.2 pM and 29 pM; little effect against PGDFR, FGFR, CSF-1, InsR and Src.
IC50 value: 5.2/29 pM(Ki/IC50) [1]
Target: EGFR
in vitro: PD 153035 shows a potent and selective inhibitory effect on tyrosine phosphorylation induced with EGF with IC50 of 15 nM and 14 nM in Swiss 3T3 fibroblast and A-431 human epidermoid carcinoma cells, respectively [1]. PD153035 shows growth inhibitory effects in cultures of EGF receptor-overexpressing human cancer cell lines including A431, Difi, DU145, MDA-MB-468 and ME180 cells with IC50 of 0.22 μM, 0.3μM, 0.4 μM, 0.68 μM and 0.95 μM, respectively [2].
in vivo: In A431 human epidermoid tumors grown as xenografts in immunodeficient nude mice, PD153035 at 80 mg/kg inhibit EGF receptor tyrosine kinase activity [3]. PD153035 improves glucose tolerance, insulin sensitivity, and signaling and reduces subclinical inflammation in HFD-fed mice [4].