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Merck
CN

PZ0191

Sigma-Aldrich

克唑替尼

≥98% (HPLC)

别名:

PF 2341066, PF-02341066, PF02341066, 克唑替尼, (R)-3-[1-(2,6-二氯-3-氟 - 苯基)-乙氧基]-5-(1-哌啶-4-基-1H-吡唑-4-基)-吡啶-2-基胺

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About This Item

经验公式(希尔记法):
C21H22Cl2FN5O
分子量:
450.34
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

检测方案

≥98% (HPLC)

形式

powder

颜色

white to tan

储存温度

room temp

SMILES字符串

C[C@@H](Oc1cc(cnc1N)-c2cnn(c2)C3CCNCC3)c4c(Cl)ccc(F)c4Cl

InChI

1S/C21H22Cl2FN5O/c1-12(19-16(22)2-3-17(24)20(19)23)30-18-8-13(9-27-21(18)25)14-10-28-29(11-14)15-4-6-26-7-5-15/h2-3,8-12,15,26H,4-7H2,1H3,(H2,25,27)/t12-/m1/s1

InChI key

KTEIFNKAUNYNJU-GFCCVEGCSA-N

基因信息

应用

克唑替尼已被用于:
  • 研究其对肝细胞生长因子受体(c-Met)表达、增殖和凋亡的影响
  • 阻断上皮细胞中神经营养性酪氨酸激酶1型受体(NTRK1)的活性
  • 恢复对厄洛替尼的敏感性

生化/生理作用

克唑替尼(PF-02341066)是受体酪氨酸激酶(RTKs)c-Met(肝细胞生长因子受体)和间变性淋巴瘤激酶(ALK)的 ATP 竞争性抑制剂。在 > 120 种研究过的不同的 RTK 中,克唑替尼是一种高度特异性的 c-Met 和 ALK 抑制剂。克里唑蒂尼被批准用于治疗具有 ALK 融合突变的非小细胞肺癌(NSCLC)亚型。

特点和优势

这种化合物是激酶磷酸酶生物学研究的特色产品。点击此处发现更多特色激酶磷酸酶生物产品。在sigma.com/discover-bsm可了解更多关于生物活性小分子的其他研究领域。

法律信息

根据Pfizer Inc的协议出售,用于研究目的。

警示用语:

Warning

危险分类

Aquatic Acute 1 - Eye Irrit. 2 - Muta. 2 - Skin Sens. 1

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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Zheng Liu et al.
Oncoimmunology, 9(1), 1758003-1758003 (2020-09-15)
Despite some of the oncogenic driver mutations that have been associated with increased expression of programmed death-ligand 1 (PD-L1), the correlation between PD-L1 expression and ROS1 fusion in NSCLC cells, especially for those with Crizotinib resistance has not been fully
Registered report: Widespread potential for growth factor-driven resistance to anticancer kinase inhibitors
Greenfield E, et al.
eLife, 3, e04037-e04037 (2014)
Shota Yamamoto et al.
Radiology, 272(2), 568-576 (2014-06-03)
To present a radiogenomic computed tomographic (CT) characterization of anaplastic lymphoma kinase (ALK)-rearranged non-small cell lung cancer (NSCLC) (ALK+). In this HIPAA-compliant institutional review board-approved retrospective study, CT studies, ALK status, and clinical-pathologic data in 172 patients with NSCLC from
Peng Liu et al.
Oncoimmunology, 9(1), 1789284-1789284 (2020-09-15)
Amid controversial reports that COVID-19 can be treated with a combination of the antimalarial drug hydroxychloroquine (HCQ) and the antibiotic azithromycin (AZI), a clinical trial (ONCOCOVID, NCT04341207) was launched at Gustave Roussy Cancer Campus to investigate the utility of this
Damini Chand et al.
Disease models & mechanisms, 6(2), 373-382 (2012-10-30)
Neuroblastoma is a childhood extracranial solid tumour that is associated with a number of genetic changes. Included in these genetic alterations are mutations in the kinase domain of the anaplastic lymphoma kinase (ALK) receptor tyrosine kinase (RTK), which have been

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