免疫法/AZD-3759/10mg 50mg 100mg/MC0949
市场价：
¥3200.00
美元价：
1600.00
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
AZD-3759
- Catalog No.：MC0949
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 1626387-80-1
- MolecularFormula：
- C22H23ClFN5O3
- Purity：
- >98%
- Target：
- EGFR
- IC50：
- IC50: 0.3 nM (EGFRwt), 0.2 nM (EGFRL858R), 0.2 nM (EGFRexon 19Del)[1]
- In Vitro：
- At 2 mM of ATP concentrations, the IC50s are 102, 7.6, and 2.4 nM for EGFRwt, EGFRL858R, and EGFRexon 19Del, respectively. AZD3759 also inhibits pEGFR in H838wt, H3255L858R, and PC-9exon 19Del with IC50 of 64.5, 7.2, and 7.4 nM, respectively. In cellular phosphorylation studies, AZD3759 also demonstrates 9-fold inhibition selectivity in EGFR-activating mutant cell lines over EGFR wild-type cell lines (H838 cell line)[1].
- In Vivo：
- Following oral dosing in rats at 2 mg/kg, absorption of AZD3759 is rapid with blood Cmax of 0.58 μM achieved at 1.0 h. Subsequently, blood concentrations of AZD3759 decline monoexponentially with a mean elimination half-life of 4.3 h, which is close to the same parameter obtained from intravenous dosing of 4.1 h. The bioavailability following an oral dose in rats is 91%. Blood pharmacokinetic parameters of AZD3759 in male dogs are determined following both a single dose intravenous infusion and oral administration. Following the IV dose in dogs, AZD3759 blood clearance is determined as 14 mL/min per kg, and the volume of distribution is 6.4 L/kg. Its elimination half-life is 6.2 h. Absorption of AZD3759 is rapid with blood Cmax (698 nM) occurring between 0.5 and 1.5 h. The oral bioavailability of AZD3759 is excellent at 90%. AZD3759 demonstrated significant dose-dependent antitumor efficacy (78% tumor growth inhibition at 7.5 mg/kg qd and tumor regression at 15 mg/kg qd, respectively,
- Fields：
- AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. IC50: 0.3 nM (EGFRwt), 0.2 nM (EGFRL858R), 0.2 nM (EGFRexon 19Del)[1]
- Specificity：
- Target: EGFR . Fields: AZD3759 is an orally available inhibitor of the epidermal growth factor receptor (EGFR), with potential antineoplastic activity. IC50: 0.3 nM (EGFRwt), 0.2 nM (EGFRL858R), 0.2 n
- Source：
- Rabbit
- Dilution：
- IC50: 0.3 nM (EGFRwt), 0.2 nM (EGFRL858R), 0.2 nM (EGFRexon 19Del)[1]
- Concentration：
- >98%
- Storage Stability：
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- Other Name：
- AZD-3759,AZD 3759,,AZD3759
- MolecularWeight(Da)：
- 459.14
- References：
- [1]. Zeng Q, et al. Discovery and Evaluation of Clinical Candidate AZD3759, a Potent, Oral Active, Central Nervous System-Penetrant, Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitor. J Med C
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