质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
room temp
InChI
1S/C24H25ClFN5O2/c1-33-22-14-20-17(24(28-15-27-20)29-16-7-8-19(26)18(25)12-16)13-21(22)30-23(32)6-5-11-31-9-3-2-4-10-31/h5-8,12-15H,2-4,9-11H2,1H3,(H,30,32)(H,27,28,29)/b6-5+
InChI key
LVXJQMNHJWSHET-AATRIKPKSA-N
生化/生理作用
达克替尼（PF-00299804）是不可逆的 EGFR 抑制剂和抗肿瘤药。 它是 HER-1（EGFR），-2 和 -4 酪氨酸激酶的有效抑制剂，对 EGFR、ERBB2 和 ERBB4 的 IC50 分别为 6.0、45.7 和 73.7 nM。 人们相信达克替尼通过在 ATP 位点结合和 erbB 家族成员催化域中亲核半胱氨酸残基的共价修饰，不可逆地抑制 erbB 酪氨酸激酶活性。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Jeffrey A Engelman et al.
Cancer research, 67(24), 11924-11932 (2007-12-20)
Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors gefitinib and erlotinib are effective treatments for a subset of non-small cell lung cancers. In particular, cancers with specific EGFR-activating mutations seem to be the most sensitive to these agents. However, despite
Yutaro Yamamoto et al.
Acta histochemica et cytochemica, 52(6), 101-106 (2020-02-01)
Dacomitinib, a second-generation tyrosine kinase inhibitor, was irreversible inhibitor forming covalent bonds with the kinase domains of EGFR and other ErbB family receptors. Dacomitinib has been approved for the treatment of locally advanced or metastatic non-small cell lung cancer. In
Andrea J Gonzales et al.
Molecular cancer therapeutics, 7(7), 1880-1889 (2008-07-09)
Signaling through the erbB receptor family of tyrosine kinases contributes to the proliferation, differentiation, migration, and survival of a variety of cell types. Abnormalities in members of this receptor family have been shown to play a role in oncogenesis, thus
Personalizing therapy in an epidermal growth factor receptor-tyrosine kinase inhibitor-resistant non-small-cell lung cancer using PF-00299804 and trastuzumab.
Ronan J Kelly et al.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 28(28), e507-e510 (2010-08-04)
Abram Calderon et al.
Oncotarget, 11(46), 4224-4242 (2020-11-28)
KSHV-associated cancers have poor prognoses and lack therapeutics that selectively target viral gene functions. We developed a screening campaign to identify known drugs that could be repurposed for the treatment of KSHV-associated cancers. We focused on primary effusion lymphoma (PEL)
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