PZ0330
达科替尼
≥98% (HPLC)
别名:
PF-00299804, PF-00299804-03, PF-299, （2E）-N- [4-[（3-氯-4-氟苯基）氨基] -7-甲氧基-6-喹唑啉基] -4-（1-哌啶基）-2-丁烯酰胺
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关于此项目
Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
room temp
SMILES string
Fc1c(cc(cc1)Nc2ncnc3c2cc(c(c3)OC)NC(=O)\C=C\CN4CCCCC4)Cl
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
Biochem/physiol Actions
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。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
商品
Discover definitions and uses for irreversible inhibitors including the types of irreversible inhibitors: suicide inhibitors, heavy metal inhibitors, and time-dependent inhibitors.
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)
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
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
全球贸易项目编号
| 货号 | GTIN |
|---|---|
| PZ0330-25MG | 04061832962696 |
| PZ0330-5MG | 04061832962702 |