CZC-8004
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货号：A114366
同义名：
CZC-00008004;Dianilinopyrimidine-01
CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase.
CZC-8004 化学结构
CZC-8004 3D分子结构
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CZC-8004 纯度/质量文件 产品仅供科研
货号：A114366
标准纯度：
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产品说明书
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CZC-8004 质控信息
转化生长因子-β 亚型比较
Bcr-Abl 亚型比较
NVP-BHG 712
+
99%+
KW-2449
+++
Abl, IC50: 14 nM
Abl (T315I), IC50: 4 nM
FLT3
99%+
Ponatinib
++++
98%
AT9283
99%+
Imatinib Mesylate
+
c-Kit,PDGFR
99%
Danusertib
++
RET
99%+
Rebastinib
++++
p-Abl1 (native), IC50: 0.75 nM
u-Abl1 (T315I), IC50: 5 nM
FLT3,Tie-2
99%+
PP121
++
VEGFR,PDGFR
99%+
GNF-7
+++
E255V, IC50: 122 nM
M351T, IC50: 133 nM
99%+
Olverembatinib dimesylate
++++
Abl, IC50: 0.34 nM
Abl (G250E), IC50: 0.35 nM
99%
Dasatinib monohydrate
++++
Src
98%
Dasatinib
++++
Src
98%
Bafetinib
+++
98+%
GNF-2
+
Bcr-Abl (K562 cell line), IC50: 273 nM
Bcr-Abl (SUP-B15 cell line), IC50: 268 nM
98%+
Degrasyn
+
DUB
98+%
GNF-5
++
98%
Radotinib
++
98+%
PD173955
Src
99%+
Nilotinib
++
98%
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
CZC-8004 生物活性
描述
Aberrant tyrosine kinase activity plays a critical role in many hematologic disorders, including chronic myeloid leukemia characterized by the constitutive activity of BCR-ABL. ABL therefore represents a crucial target for new therapeutic strategies[3] 50 values for tyrosine kinase including ABL kinase. A 50% bead loading gave the highest level of PK (protein kinase) identification for CZC-8004, extracting 55 PKs from a single cell lysate. The CZC-8004 beads extracted 61 and 64 PKs with 55 PKs common across the two bead batches examined[4]
CZC-8004 参考文献
[1] CZC-8004 is a pan-kinase inhibitor, with low micromolar IC50 values for tyrosine kinase.
[2] Bantscheff M, et al. Quantitative chemical proteomics reveals mechanisms of action of clinical ABL kinase inhibitors. Nat Biotechnol. 2007 Sep;25(9):1035-44.
[3] Cilloni D, Saglio G. Molecular pathways: BCR-ABL. Clin Cancer Res. 2012 Feb 15;18(4):930-7.
[4] Deane FM, Lin AJS, Hains PG, Pilgrim SL, Robinson PJ, McCluskey A. FD5180, a Novel Protein Kinase Affinity Probe, and the Effect of Bead Loading on Protein Kinase Identification. ACS Omega. 2017 Jul 31;2(7):3828-3838.
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CZC-8004 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
3.23mL
0.65mL
0.32mL
16.16mL
3.23mL
1.62mL
32.33mL
6.47mL
3.23mL
CZC-8004 技术信息
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