CAS NO: | 1508250-71-2 |
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 |
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] |
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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 |
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溶解性数据 | In Vitro: DMSO : ≥ 242 mg/mL(488.87 mM) *"≥" means soluble, but saturation unknown. 配制储备液
* 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。 |