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Merck

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號碼:
分類程式碼代碼:
12352200
PubChem物質ID:
NACRES:
NA.77

化驗

≥98% (HPLC)

形狀

powder

顏色

white to tan

儲存溫度

room temp

SMILES 字串

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 密鑰

KTEIFNKAUNYNJU-GFCCVEGCSA-N

基因資訊

應用

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。

特點和優勢

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。

法律資訊

根据Pfizer Inc的协议出售,用于研究目的。

訊號詞

Warning

危險分類

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3

閃點(°F)

Not applicable

閃點(°C)

Not applicable


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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
Registered report: Widespread potential for growth factor-driven resistance to anticancer kinase inhibitors
Greenfield E, et al.
eLife, 3, e04037-e04037 (2014)
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
Neurotrophic tyrosine kinase receptor 1 is a direct transcriptional and epigenetic target of IL-13 involved in allergic inflammation
Rochman M, et al.
Mucosal Immunology, 8(4), 785-785 (2015)
Nicole R Infarinato et al.
Cancer discovery, 6(1), 96-107 (2015-11-12)
Neuroblastomas harboring activating point mutations in anaplastic lymphoma kinase (ALK) are differentially sensitive to the ALK inhibitor crizotinib, with certain mutations conferring intrinsic crizotinib resistance. To overcome this clinical obstacle, our goal was to identify inhibitors with improved potency that

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