2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis
  4. ZW-49

ZW-49 是一种具有口服活性的泛 EGFR 抑制剂，其 IC50 值为 0.03-1.5 nM。ZW-49 可抑制所有 EGFR 突变亚群，且相对于野生型 EGFR 及其他靶标家族具有选择性。ZW-49 可阻断 ATP 结合口袋，占据保守的疏水亚口袋，避免与 PACC 突变 P 环产生空间位阻冲突。ZW-49 可抑制癌细胞增殖，诱导 G0/G1 期细胞周期阻滞及细胞凋亡 (apoptosis)，并在异种移植小鼠模型中展现出抗增殖活性。ZW-49 可用于癌症研究，例如非小细胞肺癌。

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ZW-49

ZW-49 Chemical Structure

CAS No. : 2055109-19-6

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ZW-49 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

查看所有亚型
EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ZW-49 is an orally active pan-EGFR inhibitor with IC50 values at 0.03-1.5 nM. ZW-49 inhibits all subgroups of EGFR mutations with selectivity over wild-type EGFR and other target families. ZW-49 blocks the ATP-binding pocket, occupies a conserved hydrophobic subpocket, avoids steric conflicts with PACC mutation P loops. ZW-49 inhibits cancer cells proliferation, induces G0/G1 phase cell-cycle arrest and apoptosis, and demonstrates anti-proliferative activity in xenograft mice models. ZW-49 can be used for the research of cancer, such as non-small cell lung cancer[1].

IC50 & Target[1]

HER2

 

体外研究
(In Vitro)

ZW-49 可强效抑制广泛的突变 EGFR 激酶组，对 EGFRL858R/T790M 的 IC50 为 1.5 nM，对野生型 EGFR 的选择性达 6.6 倍 (IC50 = 9.9 nM)，同时还可靶向特定的 HER2 突变体[1]。
ZW-49 (72 h) 可强效抑制 EGFR 突变细胞系的增殖，包括 NCI-H1975 (IC50 = 12 nM) 和 HCC827 (IC50 = 4 nM)，同时也能作用于携带非经典 EGFR 突变的 Ba/F3 细胞 (IC50 = 0.58-5.59 nM)，还可抑制 HER2 过表达细胞[1]。
ZW-49 (1-1000 nM; 2 h) 可在 EGFR 突变细胞系中强效且呈剂量依赖性地抑制 EGFR 磷酸化及下游 AKT/ERK 信号通路，这些细胞系包括表达非经典突变的 NCI-H1975、HCC827 和 Ba/F3 细胞[1]。
ZW-49 (0.01-1 μM) 可诱导 H1975 细胞发生 G0/G1 期细胞周期阻滞及凋亡[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

ZW-49 相关抗体:

Western Blot Analysis[1]

Cell Line: Cancer cell lines (NCI-H1975, HCC827, Ba/F3 with EGFR G719A and D770-N771insNPG, A431)
Concentration: 1, 10, 100, 1000 nM
Incubation Time: 2 h
Result: Completely abrogated phosphorylation of EGFR, AKT, and ERK in NCI-H1975 and HCC827 cells at 10 nM.
Exerted dose-dependent inhibition of p-EGFR, p-AKT, and p-ERK at concentrations from 1 to 1000 nM in Ba/F3 cells expressing EGFR G719A and D770-N771insNPG, while total protein levels remained stable.
Inhibited EGFR phosphorylation and downstream signaling in A431 cells at 100 nM.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ F
Rat[1] 1 mg/kg i.v. 2.32 h 0.08 h 215.17 ng/mL 341.02 ng·h/mL / /
Rat[1] 10 mg/kg i.g. 4 h 4 h 50.62 ng/mL 275.1 ng·h/mL 442.64 ng·h/mL 8.73 %
体内研究
(In Vivo)

ZW-49 (5-25 mg/kg；口服；每日 1 次；2 周) 可抑制多种癌细胞异种移植小鼠模型中的肿瘤生长[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c (nu/nu) mice (4–6 weeks old) xenograft models bearing H1975, BaF3-EGFR D770-N771insNPG, BaF3-EGFR G719A, or A431 cell lines[1]
Dosage: p.o.; qd; 2 weeks
Administration: p.o.; qd; 2 weeks
Result: Reduced tumor volume.
Showed no significant weight change and obvious pathological changes.
Reduced phosphorylated EGFR levels and p-AKT and p-ERK levels.
分子量

588.66

Formula

C33H32N8O3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

ZW-49 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ZW-492055109-19-6ZW49ZW 49EGFRApoptosisEpidermal growth factor receptorErbB-1HER1male Sprague-Dawley ratsG0/G1 phase cell-cycle arrestapoptosisNCI-H1975ERK signaling pathwaysnon-small cell lung cancerHER2AKTATP-binding pocketInhibitorinhibitorinhibit

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