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Nazartinib
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nazartinib图片
CAS NO:1508250-71-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
200mg电议
500mg电议

产品名称
那扎替尼
EGF816
产品介绍
Nazartinib (EGF816) 是一种EGFR抑制剂,对 EGFR(L858R/790M) 突变体的KiKinact值分别为 31 nM 和 0.222 min–1
生物活性

Nazartinib (EGF816) is a covalent mutant-selectiveEGFRinhibitor, withKiandKinactof 31 nM and 0.222 min–1on EGFR(L858R/790M) mutant, respectively.

IC50& Target[1]

EGFRL858R/T790M

31 nM (Ki)

体外研究
(In Vitro)

Nazartinib (EGF816) has inhibitory effect on the mutant cell lines with IC50s of 4, 6, 2 nM in H1975, H3255, and HCC827, respectively, and demonstrates improved ADME and PK properties[1]. Nazartinib (EGF816) shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 cell lines with EC50values of 5, 1, and 3 nM, respectively. Nazartinib inhibits cell proliferation, with EC50values of 9, 11, and 25 nM in H3255, HCC827, and H1975, respectively. Nazartinib has an OC50(compound concentration at 50% occupancy) value of 2 and 5 nM on HCC827 and H1975, respectively[2].

体内研究
(In Vivo)

In H1975 mouse xenograft model, Nazartinib (EGF816; 50 and 20 mg/kg or 25 mg/kg, p.o.) demonstrates dose-dependent efficacy with near complete tumor cells regression at the highest dose tested (50 mg/kg)[1]. In H1975 mouse model, Nazartinib (EGF816; 10 mg/kg, p.o.) induces tumor growth inhibition with a T/C (tumor/control volume) of 29%, and when doses are 30 and 100 mg/kg, tumor regressions are achieved (T/C, -61% and -80%, respectively). In the H3255 xenograft model, Nazartinib (30 mg/kg, p.o.) shows significant antitumor activity. Antiproliferative activity of Nazartinib on 89 lung cancer cell lines indicates that Nazartinib selectively inhibits cell lines containing EGFR with catalytic domain mutations[2].

Clinical Trial
分子量

495.02

性状

Solid

Formula

C26H31ClN6O2

CAS 号

1508250-71-2

中文名称

那扎替尼

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : ≥ 242 mg/mL(488.87 mM)

*"≥" means soluble, but saturation unknown.

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.0201 mL10.1006 mL20.2012 mL
5 mM0.4040 mL2.0201 mL4.0402 mL
10 mM0.2020 mL1.0101 mL2.0201 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。