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质量水平
检测方案
≥98% (HPLC)
形式
powder
颜色
white to beige
溶解性
DMSO: 5 mg/mL, clear (warmed)
储存温度
room temp
SMILES字符串
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
InChI key
KTEIFNKAUNYNJU-LBPRGKRZSA-N
生化/生理作用
（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。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°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
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
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
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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