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产品名称 | HER2 ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Poziotinib |
++++
HER2, IC50: 5.3 nM |
98% | |||||||||||||||||
Tyrphostin AG 879 |
+
HER2-Neu, IC50: 1.0 μM |
95% | |||||||||||||||||
TAK-285 |
+
HER2, IC50: 17 nM |
99%+ | |||||||||||||||||
ARRY-380 analog | ✔ | 99% | |||||||||||||||||
Canertinib |
+++
ErbB2, IC50: 9.0 nM |
EGFR | 99%+ | ||||||||||||||||
(E/Z)-CP-724714 |
++
HER2/ErbB2, IC50: 10 nM |
95% | |||||||||||||||||
Lapatinib |
+++
ErbB2, IC50: 9.2 nM |
EGFR | 98% | ||||||||||||||||
AEE788 |
++++
HER2/ErbB2, IC50: 6 nM |
EGFR | 98+% | ||||||||||||||||
Neratinib |
+
HER2, IC50: 59 nM |
Src,EGFR | 98% | ||||||||||||||||
BMS-599626 |
+
HER2, IC50: 30 nM |
98% | |||||||||||||||||
Mubritinib |
++++
HER2/ErbB2, IC50: 6.0 nM |
99%+ | |||||||||||||||||
Tucatinib |
+++
ErbB2, IC50: 8 nM |
98% | |||||||||||||||||
Sapitinib |
++++
ErbB2, IC50: 3 nM |
EGFR | 99%+ | ||||||||||||||||
CUDC-101 |
++
HER2, IC50: 15.7 nM |
HDAC,EGFR | 99%+ | ||||||||||||||||
Afatinib dimaleate |
++
HER2, IC50: 14 nM |
98% | |||||||||||||||||
Afatinib |
++
HER2, IC50: 14 nM |
99% | |||||||||||||||||
Pertuzumab | ✔ | 95% | |||||||||||||||||
Trastuzumab | ✔ | 99% | |||||||||||||||||
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。 |
描述 | TAS0728 is a potent, selective, orally active, irreversible and covalently bound HER2 inhibitor with an IC50 of 13 nM. The IC50s of TAS0728 against BMX, HER4, BLK, EGFR, JAK3, SLK, and LOK were 4.9, 8.5, 31, 65, 33, 25, and 86 nM respectively. In addition, TAS0728 inhibited HER2, HER4, BLK, EGFR, JAK3 and LOK with an IC50 of 4.9, 8.5, 31, 65, 33, 25, and 86 nM. TAS0728 potently and consistently inhibited the phosphorylation of HER2, HER3 and downstream effectors. In the HER2-amplified SK-BR-3/AU565/BT-474/NCI-N87/Calu-3 cell line, TAS0728 showed antiproliferative effects with GI50 values of 5.0/5.1/3.6/1.6/6.9 nM, respectively[1]. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.98mL 0.40mL 0.20mL |
9.91mL 1.98mL 0.99mL |
19.82mL 3.96mL 1.98mL |
CAS号 | 2088323-16-2 |
分子式 | C26H32N8O3 |
分子量 | 504.58 |
SMILES Code | [H][C@]1(CCCN(C(C=C)=O)C1)N2C3=NC=NC(N)=C3C(C(NC4=C(C)C(C)=C(CC(N(C)C)=O)C=C4)=O)=N2 |
MDL No. | MFCD31813813 |
别名 | TPC 107 |
运输 | 蓝冰 |
InChI Key | JCCIICHPRAAMGK-GOSISDBHSA-N |
Pubchem ID | 130275856 |
存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C |
溶解方案 |
DMSO: 120 mg/mL(237.82 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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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