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Merck
CN

PZ0271

Sigma-Aldrich

醋酸PF-06463922

≥98% (HPLC)

别名:

醋酸洛拉替尼, (10R).7-氨基-12-氟-2,10,16-三甲基-15-氧代-10,15,16,17-四氢-2H.8,4-(甲基)吡唑并[4,3.h ] [2,5,11]-苯并二氮杂二环十四癸-3-乙酸乙腈

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About This Item

经验公式(希尔记法):
C21H19FN6O2 · CH3COOH
分子量:
466.46
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77

质量水平

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 10 mg/mL, clear

储存温度

room temp

SMILES字符串

CC(O)=O.NC1=C(O[C@@H](C2=C3C=CC(F)=C2)C)C=C(C4=C(C#N)N(C)N=C4CN(C)C3=O)C=N1

InChI

1S/C21H19FN6O2.C2H4O2/c1-11-15-7-13(22)4-5-14(15)21(29)27(2)10-16-19(17(8-23)28(3)26-16)12-6-18(30-11)20(24)25-9-12;1-2(3)4/h4-7,9,11H,10H2,1-3H3,(H2,24,25);1H3,(H,3,4)/t11-;/m1./s1

InChI key

BLNAIBLTPYGILH-RFVHGSKJSA-N

应用

PF-06463922乙酸已被用作间变性淋巴瘤激酶(ALK)的抑制剂,从而通过qPCR对肾上腺髓质素的表达进行分析。

生化/生理作用

PF-06463922是变性淋巴瘤激酶(ALK)和c-ros癌基因1(ROS1)的一种有效的选择性脑可穿透抑制剂,其对在克唑替尼耐药的患者中发现的所有已知ALK和ROS1突变体均具有很强的活性。PF-06463922正被用于治疗非小细胞肺癌(NSCLC)的临床试验中。

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


历史批次信息供参考:

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Shana Claeys et al.
Oncotarget, 8(63), 106820-106832 (2018-01-02)
Neuroblastoma is an aggressive childhood malignancy of the sympathetic nervous system. Despite multi-modal therapy, survival of high-risk patients remains disappointingly low, underscoring the need for novel treatment strategies. The discovery of Here, we further dissected the transcriptional dynamic profiles of
Early and late effects of pharmacological ALK inhibition on the neuroblastoma transcriptome
Shana Claeys
Oncotarget (2017)
Liying Chen et al.
The Journal of clinical investigation, 128(1), 446-462 (2017-12-05)
Pharmacologically difficult targets, such as MYC transcription factors, represent a major challenge in cancer therapy. For the childhood cancer neuroblastoma, amplification of the oncogene MYCN is associated with high-risk disease and poor prognosis. Here, we deployed genome-scale CRISPR-Cas9 screening of

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