Ambeed.cn

首页 / / / EGFR / Firmonertinib mesylate

甲磺酸伏美替尼 /Firmonertinib mesylate 99%+

货号:A1176940 同义名: Alflutinib mesylate;Furmonertinib mesylate Ambeed 开学季,买赠积分,赢豪礼

AST2818 mesylate is an EGFR inhibitor.

Firmonertinib mesylate 化学结构 CAS号:2130958-55-1
Firmonertinib mesylate 化学结构
CAS号:2130958-55-1
Firmonertinib mesylate 3D分子结构
CAS号:2130958-55-1
Firmonertinib mesylate 化学结构 CAS号:2130958-55-1
Firmonertinib mesylate 3D分子结构 CAS号:2130958-55-1
规格 价格 会员价 库存 数量
{[ item.pr_size ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb_sale, 1,1) ]}

{[ getRatePrice(item.pr_rmb, 1,1) ]}

{[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]}
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} 现货 咨询 - +
购物车0 收藏 询单

Firmonertinib mesylate 纯度/质量文件 产品仅供科研

货号:A1176940 标准纯度: 99%+
批次查询: 批次纯度:

全球学术期刊中引用的产品

Cell,2024. Ambeed. [ A125712 ]
Cancer Discov., 2024. Ambeed. [ A285925 ]
JMC, 2024, 67(17): 14974-14985. Ambeed. [ A288696 ]
JMC, 2024, 67(17): 15061-15079. Ambeed. [ A524399 , A633512 , A144280 , A174613 ]
EJNMMI Radiopharm. Chem., 2024, 9, 61. Ambeed. [ A1257961 , A622068 ]
更多 >
产品名称 EGFR/ErbB1 ErbB3 ErbB4 HER2/ErbB2 mutant EGFR 其他靶点 纯度
WZ-3146 ++++

EGFR (E746_A750/T790M), IC50: 14 nM

EGFR (E746_A750), IC50: 2 nM

99%+
Daphnetin +

EGFR, IC50: 7.67 μM

PKA,PKC 95%
Lifirafenib ++

EGFR, IC50: 29 nM

+

EGFR(T790M/L858R), IC50: 495 nM

96%
PD168393 ++++

EGFR, IC50: 0.70 nM

99%+
Nazartinib ++

mutant EGFR, Ki: 0.031 μM

++

mutant EGFR, Ki: 0.031 μM

98%
Norcantharidin 98%
CL-387785 ++++

EGFR, IC50: 370 pM

98%
WHI-P154 +++

EGFR, IC50: 4 nM

VEGFR,Src 98%
Tyrphostin A9 +

EGFR, IC50: 460 μM

PDGFR 98%
AG 555 +

EGFR, IC50: 0.7 μM

98%
AG 494 +

EGFR, IC50: 1.2 μM

99%+
AG-556 +

EGFR, IC50: 5 μM

98%
RG13022 +

EGFR, IC50: 4 μM

99%+
Tyrphostin RG 14620 99%+
Vandetanib +

EGFR, IC50: 500 nM

98%
CNX-2006 ++

mutant EGFR, IC50: <20 nM

++

mutant EGFR, IC50: <20 nM

98%
AZD3759 ++++

EGFR (L858R), IC50: 0.2 nM

EGFR (WT), IC50: 0.3 nM

98%
Erlotinib ++++

EGFR, IC50: 2 nM

95%
Saracatinib +++

EGFR, IC50: 5 nM

EGFR (L861Q), IC50: 4 nM

99%+
AG1557 98%
Rociletinib ++

EGFR (L858R/T790M), Ki: 21.5 nM

EGFR (wt), Ki: 303.3 nM

98%
AG490 +

EGFR, IC50: 0.1 μM

98%
Cetuximab ++++

EGFR, Kd: 0.39 nM

95%
Osimertinib ++

WT EGFR, IC50: 12.92 nM

L858R/T790M EGFR, IC50: 11.44 nM

99%
Osimertinib mesylate 98% (Content MsOH 15.2-18.2%)
Chrysophanol mTOR 98%
PD153035 ++++

EGFR, Ki: 5.2 pM

99%+
Olmutinib BTK 99%+
WZ4002 ++++

EGFR (L858R), IC50: 2 nM

EGFR (L858R/T790M), IC50: 8 nM

99%+
Icotinib +++

EGFR, IC50: 5 nM

98+%
Desmethyl Erlotinib HCl ++++

EGFR, IC50: 2 nM

98%
Cyasterone 99%+
PP 3 +

EGFR tyrosine kinase, IC50: 2.7 μM

98%
WZ8040 99%+
(-)-Epigallocatechin Gallate 99%
AG 18 +

EGFR, IC50: 35 μM

99%+
O-Desmethyl gefitinib ++

EGFR, IC50: 36 nM

98%
Falnidamol 99%+
AZ-5104 ++++

EGFR (L858R), IC50: 6 nM

EGFR (L861Q) , IC50: <1 nM

+++

ErbB4, IC50: 7 nM

BRK 99%+
Butein 95%
Genistein 98%
SU5214 +

EGFR, IC50: 36.7 μM

99%+
Naquotinib 99%+
Gefitinib ++

EGFR, IC50: 15.5 nM

+

EGFR (858R/T790M), IC50: 823.3 nM

98%
Theliatinib +++

WT EGFR, IC50: 3 nM

++

EGFR T790M/L858R, IC50: 22 nM

98+%
Lazertinib ++++

WT EGFR, IC50: 76 nM

L858R/T790M EGFR, IC50: 2 nM

++++

Del19/T790M, IC50: 1.7 nM

99%+
Gefitinib-based PROTAC 3 ++

EGFR, DC50: 22.3 nM

99%+
MTX-211 PI3K 98%
(E)-AG 99 99%+
Licochalcone D PARP,Caspase 97%
Zipalertinib +++

EGFR WT, IC50: 8 nM

EGFR (L861Q), IC50: 4.1 nM

+++

HER4, IC50: 4 nM

++++

EGFR L858R, IC50: 2 nM

EGFR(d746-750), IC50: 1.4 nM

97%
JND3229 +++

EGFR WT, IC50: 6.8 nM

++

EGFR L858R/T790M, IC50: 30.5 nM

99%+
Firmonertinib mesylate 99%+
Tyrphostin AG30 99%+
EGFR-IN-12 ++

EGFR, IC50: 21 nM

99%+
Mobocertinib 98%
(Rac)-JBJ-04-125-02 99%
(S)-Sunvozertinib 98%
BLU-945 95%
Poziotinib +++

HER1, IC50: 3.2 nM

++

HER4, IC50: 23.5 nM

+++

HER2, IC50: 5.3 nM

98%
TAK-285 ++

EGFR/HER1, IC50: 23 nM

+

HER4, IC50: 260 nM

++

HER2, IC50: 17 nM

99%+
ARRY-380 analog 98%
Canertinib ++++

EGFR, IC50: 1.5 nM

+++

ErbB2, IC50: 9.0 nM

99%+
Dacomitinib +++

EGFR, IC50: 6.0 nM

+

ErbB4, IC50: 73.7 nM

+

ErbB2, IC50: 45.7 nM

98%
EGFR/ErbB-2/ErbB-4 inhibitor-2 +

ErbB4, IC50: 1.91 μM

+

ErbB2, IC50: 0.08 μM

99%+
(E/Z)-CP-724714 ++

HER2/ErbB2, IC50: 10 nM

98+%
Lapatinib ++

EGFR, IC50: 10.8 nM

+

ErbB4, IC50: 367 nM

+++

ErbB2, IC50: 9.2 nM

98%
AEE788 ++++

EGFR, IC50: 2 nM

+

HER4/ErbB4, IC50: 160 nM

+++

HER2/ErbB2, IC50: 6 nM

c-Fms 98+%
AV-412 free base ++++

EGFR, IC50: 0.75 nM

++

ErbB2, IC50: 19 nM

++++

EGFRT790M, IC50: 0.79 nM

EGFRL858R/T790M, IC50: 0.51 nM

98+%
Neratinib +

EGFR, IC50: 92 nM

+

HER2, IC50: 59 nM

Src 98%
BMS-599626 ++

HER1, IC50: 20 nM

+

HER4, IC50: 190 nM

++

HER2, IC50: 30 nM

99+%
Tucatinib +++

ErbB2, IC50: 8 nM

98%
Allitinib ++++

EGFR, IC50: 0.5 nM

++++

ErbB4, IC50: 0.8 nM

+++

ErbB2, IC50: 3.0 nM

99%
Pelitinib +

EGFR, IC50: 38.5 nM

+

ErbB2, IC50: 1.255 μM

Src,Raf 99%+
Sapitinib +++

EGFR, IC50: 4 nM

+++

ErbB3, IC50: 4 nM

+++

ErbB2, IC50: 3 nM

99%+
CUDC-101 +++

EGFR, IC50: 2.4 nM

++

HER2, IC50: 15.7 nM

HDAC 99%+
Varlitinib +++

ErbB1, IC50: 7 nM

++++

ErbB2, IC50: 2 nM

99%+
Afatinib dimaleate ++++

EGFR (wt), IC50: 0.5 nM

EGFR (L858R/T790M), IC50: 0.4 nM

++

HER2, IC50: 14 nM

98%
Canertinib dihydrochloride +++

EGFR, IC50: 7.4 nM

+++

ErbB2, IC50: 9 nM

98%
Allitinib tosylate ++++

EGFR (T790M/L858R), IC50: 12 nM

EGFR, IC50: 0.5 nM

++++

ErbB4, IC50: 0.8 nM

+++

ErbB2, IC50: 3.0 nM

99%
Tyrphostin AG 528 +

EGFR, IC50: 4.9 μM

+

HER2, IC50: 2.1 μM

98%
Afatinib ++++

EGFR (wt), IC50: 0.5 nM

EGFR (L858R), IC50: 10 nM

++++

ErbB4, IC50: 1 nM

++

HER2, IC50: 14 nM

99%
Pyrotinib dimaleate ++

EGFR, IC50: 0.013 μM

++

HER2, IC50: 0.038 μM

98%
Epertinib HCl ++++

EGFR, IC50: 1.48 nM

+++

HER4, IC50: 2.49 nM

+++

HER2, IC50: 7.15 nM

98%
Tuxobertinib ++++

EGFR, Kd: 0.2 nM

++++

HER2, Kd: 0.76 nM

98%
ALK-IN-1 ++

EGFR(C797S/del19), IC50: 138.6 nM

EGFR(del19), IC50: 36.8 nM

ALK 98+%
Brigatinib +

EGFR(del19), IC50: 39.9 nM

EGFR(C797S/T790M/del19), IC50: 67.2 nM

ALK,FLT3 98%
Avitinib ++++

EGFR L858R/T790M, IC50: 0.18 nM

BTK 99%+
EAI045 97%
Almonertinib 98%
BI-4020 ++++

EGFRdel19 T790M C797S, IC50: 0.2 nM

99%+
EGFR-IN-7 ++++

EGFRd746-750/T790M/C797S, IC50: 0.26 nM

EGFRL858R/T790M, IC50: 0.19 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Firmonertinib mesylate 生物活性

靶点
  • EGFR/ErbB1

描述 Non-small-cell lung cancer (NSCLC) accounts for approximately 85% of all types of lung cancer. The first- and second-generation EGFR tyrosine kinase inhibitors (TKIs) have been recommended as the first-line therapy for patients with EGFR mutation-positive NSCLC. But almost all patients eventually developed clinical resistance which led to the development of third-generation EGFR-TKIs. AST2818 is a newly developed third-generation EGFR-TKI selective for EGFR-sensitizing and T790M-resistant mutations. AST2818 has a pharmacologically active metabolite, AST5902, which has similar antitumor activity [1]. Nude mice (expressing EGFR L858R and T790M) were treated with AST2818 through gavage once daily [QD] for 28 d. The average tumor growth inhibition was achieved in the 10 and 30 mg/kg AST2818 by 87% and 100%, respectively. Furthermore, AST2818 was safe and well tolerated at daily doses up to 240 mg in patients with advanced NSCLC with confirmed EGFR T790M mutation. The 80 mg daily dose of AST2818 had prolonged antitumor activity in patients with NSCLC [2]. At present, AST2818 has undergone phase II/III clinical trials for non-small cell lung cancer (NSCLC) treatment in China [3].

Firmonertinib mesylate 参考文献

[1]Shi Y. Safety, Clinical Activity, and Pharmacokinetics of Alflutinib (AST2818) in Patients With Advanced NSCLC With EGFR T790M Mutation. J Thorac Oncol. 2020 Jun;15(6):1015-1026.

[2] Shi Y. Safety, Clinical Activity, and Pharmacokinetics of Alflutinib (AST2818) in Patients With Advanced NSCLC With EGFR T790M Mutation. J Thorac Oncol. 2020 Jun;15(6):1015-1026.

[3]Liu X. Simultaneous determination of alflutinib and its active metabolite in human plasma using liquid chromatography-tandem mass spectrometry. J Pharm Biomed Anal. 2019 Nov 30;176:112735. doi: 10.1016/j.jpba.2019.06.032.

Firmonertinib mesylate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.50mL

0.30mL

0.15mL

7.52mL

1.50mL

0.75mL

15.04mL

3.01mL

1.50mL

Firmonertinib mesylate 技术信息

CAS号2130958-55-1
分子式C29H35F3N8O5S
分子量 664.699
别名 Alflutinib mesylate;Furmonertinib mesylate;AST2818;Alflutinib (mesylate);AST2818 mesylate
运输蓝冰
存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 4 mg/mL(6.02 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
Ambeed 相关网站 Ambeed.cn Ambeed.com
Ambeed
关于我们
联系我们
资讯中心
网站地图
产品手册
  • 批次文件查询
  • 客户支持
    专业术语
    缩略词释义
    质量手册
    产品咨询
    计算器
    活动政策
    订购方法
    活动声明
    联系我们
    400-920-2911 sales@ambeed.cn tech@ambeed.cn
    Ambeed 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务,不为任何个人或者非科研性质用途提供服务。