PZ0240
（S）-克罗替尼
≥98% (HPLC)
别名:
3-[（1S）-1-（2,6-二氯-3-氟苯基）乙氧基] -5- [1-（4-哌啶基）-1H-吡唑-4-基] -2-吡啶胺
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选择尺寸
关于此项目
经验公式（希尔记法）:
C21H22Cl2FN5O
化学文摘社编号:
分子量:
450.34
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
InChI key
KTEIFNKAUNYNJU-LBPRGKRZSA-N
SMILES string
ClC1=C([C@H](C)OC2=C(N)N=CC(C3=CN(C4CCNCC4)N=C3)=C2)C(Cl)=C(F)C=C1
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-/m0/s1
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 5 mg/mL, clear (warmed)
storage temp.
room temp
Quality Level
Biochem/physiol Actions
（S）-克唑替尼与其（R）-对映异构体（临床批准的抗癌药Xalkori）具有明显不同的特征。（S）-克唑替尼不是靶向ALK、MET和ROS1的药物，而是一种对人7,8-二氢-8-氧鸟嘌呤三磷酸酶MTH1（NUDT1）具有高度选择性的抑制剂，其IC50 值为330 nM，与临床使用的（R）-异构体相比，对MTH1的亲和力高16倍。 MTH1可水解氧化的嘌呤核苷三磷酸，否则它们可能会掺入DNA/RNA中并造成DNA损伤。MTH1可去除因快速增殖的癌细胞中活性氧（ROS）水平升高而产生的氧化核苷酸，有助于保护癌细胞免受增殖压力并防止癌细胞的死亡。它被认为是癌症治疗的新靶标。在使用SW480细胞的小鼠异种移植研究中，（S）-克唑替尼（而非其（R）-对映异构体）能够破坏总体的肿瘤进展，并且可特异性地将肿瘤体积减少50％以上。
（S）-克唑替尼是人7,8-二氢-8-氧鸟嘌呤三磷酸酶MTH1（NUDT1）的一种高度选择性抑制剂。
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Huaping Chen et al.
International journal of molecular sciences, 21(22) (2020-11-27)
MTH1 (MutT homolog 1) or NUDT1 (Nudix Hydrolase 1), also known as oxidized purine nucleoside triphosphatase, has potential as a biomarker for monitoring cancer progression and quantifying target engagement for relevant therapies. In this study, we validate one MTH1 inhibitor
Melike Çağlayan et al.
Nature communications, 8, 14045-14045 (2017-01-10)
Oxidative stress in cells can lead to accumulation of reactive oxygen species and oxidation of DNA precursors. Oxidized purine nucleotides can be inserted into DNA during replication and repair. The main pathway for correcting oxidized bases in DNA is base
Xuanxuan Dai et al.
Journal of experimental & clinical cancer research : CR, 36(1), 120-120 (2017-09-09)
Non-small cell lung cancer (NSCLC) accounts for approximately 80-85% of all lung cancers and is usually diagnosed at an advanced stage with poor prognosis. Targeted therapy has produced unprecedented outcomes in patients with NSCLC as a number of oncogenic drivers
Peng Liu et al.
Nature communications, 10(1), 1486-1486 (2019-04-04)
Immunogenic cell death (ICD) converts dying cancer cells into a therapeutic vaccine and stimulates antitumor immune responses. Here we unravel the results of an unbiased screen identifying high-dose (10 µM) crizotinib as an ICD-inducing tyrosine kinase inhibitor that has exceptional antineoplastic
Stefan Nagel et al.
Oncotarget, 11(34), 3208-3226 (2020-09-15)
NKL homeobox genes encode developmental transcription factors and display an NKL-code according to their physiological expression pattern in hematopoiesis. Here, we analyzed public transcriptome data from primary innate lymphoid cells (ILCs) for NKL homeobox gene activities and found that ILC3
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