CZC-8004 | CZC-00008004 | pan-kinase Inhibitor | AmBeed-信号通路专用抑制剂

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CZC-8004 95%

货号：A114366 同义名： CZC-00008004;Dianilinopyrimidine-01 产品仅供科研

CZC-8004 is a pan-kinase inhibitor and binds a range of tyrosine kinases, including ABL kinase.

CZC-8004 化学结构
CAS号：916603-07-1

CZC-8004 3D分子结构
CAS号：916603-07-1

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CZC-8004 纯度/质量文件

货号：A114366 标准纯度：95% 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Mar. Drugs, 2024, 22(5): 194. Ambeed. [ A104599 ]; • Pharmaceuticals, 2024, 17(5): 570. Ambeed. [ A224421 ]; 更多 >

转化生长因子-β 亚型比较
Bcr-Abl 亚型比较

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								99%+
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		99%+
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		98%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 nM		99%+
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。

产品名称	Abl ↓ ↑	Bcr-Abl ↓ ↑	其他靶点	纯度
NVP-BHG 712	+ c-Abl, IC50: 1.667 μM			99%+
KW-2449	+++ Abl (T315I), IC50: 4 nM Abl, IC50: 14 nM		FLT3	99%+
Ponatinib	++++ Abl, IC50: 0.37 nM			98%
AT9283				99%+
Imatinib Mesylate	+ v-Abl, IC50: 600 nM		PDGFR,c-Kit	99%
Danusertib	++ Abl, IC50: 25 nM		RET	99%+
Rebastinib	++++ u-Abl1 (T315I), IC50: 5 nM p-Abl1 (native), IC50: 0.75 nM		FLT3,Tie-2	99%+
PP121	++ Abl, IC50: 18 nM		PDGFR,VEGFR	99%+
GNF-7	+++ M351T, IC50: 133 nM E255V, IC50: 122 nM			99%+
Olverembatinib dimesylate	++++ Abl, IC50: 0.34 nM Abl (G250E), IC50: 0.35 nM			99%
Dasatinib monohydrate	++++ Abl , IC50: 0.6 nM		Src	98%
Dasatinib	++++ Abl, IC50: 0.6 nM		Src	98%
Bafetinib	+++ Abl, IC50: 5.8 nM			99%+
GNF-2		+ Bcr-Abl (SUP-B15 cell line), IC50: 268 nM Bcr-Abl (K562 cell line), IC50: 273 nM		98%+
Degrasyn		+ Bcr-Abl, IC50: 1.8 μM	DUB	99%+
GNF-5		++ Bcr-Abl, IC50: 220 nM		98%
Radotinib		++ BCR-ABL1, IC50: 34 nM		98+%
PD173955			Src	99%+
Nilotinib		++ Bcr-Abl, IC50: <30 nM		98%
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]. CZC-8004 is a pan-kinase inhibitor, with low micromolar IC₅₀ 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.

CZC-8004 实验方案

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

CAS号	916603-07-1
分子式	C₁₇H₁₆FN₅
分子量	309.341

别名	CZC-00008004;Dianilinopyrimidine-01
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 80 mg/mL(258.61 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

CZC-8004 95%

CZC-8004 纯度/质量文件

全球学术期刊中引用的产品

CZC-8004 生物活性

CZC-8004 参考文献

CZC-8004 实验方案

CZC-8004 技术信息

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CZC-8004 95%

CZC-8004 纯度/质量文件

全球学术期刊中引用的产品

CZC-8004 生物活性

CZC-8004 参考文献

CZC-8004 实验方案

CZC-8004 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

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