2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. GW2974

GW2974 

目录号: HY-112293 纯度: 99.54%
COA 产品使用指南

摩尔计算器

GW2974 是一种强效的 EGFR 和 HER2 双抑制剂，其 IC50 值分别为0.007 μM 和0.016 μM。GW2974 对 EGFR 和 HER2 的结构域具有体外抑制作用，并抑制肿瘤细胞的生长，可用于胶质母细胞瘤 (GBM) 疾病的研究。

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GW2974 Chemical Structure

GW2974 Chemical Structure

CAS No. : 202272-68-2

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10 mg ￥1950
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GW2974 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GW2974 is a potent dual inhibitor of EGFR and HER2 with IC50 value of 0.007 μM and 0.016 μM, respectively. GW2974 demonstrates in vitro inhibition of the EGFR and HER2 and inhibits the growth of tumor cell. GW2974 can be used for glioblastoma multiforme (GBM) disease research[1][2].

IC50 & Target[2]

EGFRL858R/T790M

0.007 μM (IC50)

HER2

0.016 μM (IC50)

体外研究
(In Vitro)

GW2974 (0.5-50 μM, 3小时) 10 μM 或以上时具有明显的细胞毒性，在 0.5-5 μM 时可抑制 U87MG 和 U251MG 细胞在 24 小时处理后的增殖[1]。
GW2974 (0.5-5 μM, 24小时) GW2974 在 GBM 细胞侵袭和迁移中的作用与剂量有关[1]。
GW2974 (0.001-100 μM, 24小时) 抑制 BT474, HN5, N87 细胞生长[2]。

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

GW2974 相关抗体:

Cell Viability Assay[1]

Cell Line: U87MG, U251MG
Concentration: 0.5-50 μM
Incubation Time: 3 h
Result: Reduced U87MG and U251MG cells viability to 89.4% and 86.3% in 0.5 μM and 5 μM compared with control.

Cell Proliferation Assay[1]

Cell Line: U87MG, U251MG
Concentration: 0.5-5 μM
Incubation Time: 24 h
Result: Inhibited U87MG and U251MG cells proliferation in 0.5 μM and 5μM.

Cell Invasion Assay[1]

Cell Line: U87MG, U251MG
Concentration: 0.5-5 μM
Incubation Time: 24 h
Result: Reduced the percentage to 55.6% and 48.6% of U87MG and U251MG cells in 0.5 μM, respectively.

Cell Migration Assay [1]

Cell Line: U87MG, U251MG
Concentration: 0.5-5 μM
Incubation Time: 24 h
Result: Decreased the relative migration distances (percentage) of U87MG and U251MG cells to 40.2% and 51.6% in 0.5 μM, respectively.
Resulted in a relative migration distances of U87MG and U251MG cells in 5 μM compared with control.

Cell Proliferation Assay[2]

Cell Line: BT474, HN5, N87
Concentration: 0.001-100 μM
Incubation Time: 24 h
Result: Inhibited cell growth by 50% at concentrations > 1.0 μM with IC50s < 0.4 μM.
体内研究
(In Vivo)

GW2974 (30 mg/kg, 100 mg/kg,口服给药，每天一次) 在低剂量 (30 mg/kg) 对GBM 小鼠颅内肿瘤的生长、侵袭和血管生成均有抑制作用，而高剂量的 GW2974 则完全消除了低剂量 GW2974 对肿瘤侵袭的抑制作用[1]。
GW2974 (10 mg/kg, 30 mg/kg,口服给药，每天两次) 在 HN5 人肿瘤异种移植小鼠模型和 BT474 人肿瘤异种移植小鼠模型中都以剂量依赖的方式显著抑制肿瘤生长[2]。

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

Animal Model: GBM xenograft mice model[1]
Dosage: 30 mg/kg, 100 mg/kg
Administration: Oral gavage (p.o.)
Result: Decelerated tumor growth at dose of 30 mg/kg and 100 mg/kg.
Inhibited the invasion to peritumor areas of tumors in 30 mg/kg group but augmented tumor invasion in 100 mg/kg group of brain tissues.
Inhibited angiogenesis in doses of 30 mg/kg and 100 mg/kg.
Animal Model: CD-1 nude mice (HN5), C.B-17 SCID mice (BT474)[2]
Dosage: 10 mg/kg, 30 mg/kg
Administration: Oral gavage (p.o.)
Result: Inhibited tumor growth in the HN5 model by treatment dose with 30 mg/kg.
Inhibited tumor growth in the HN5 model about 95% inhibition and BT474 model about 50% inhibition by treatment dose with 10 mg/kg.
分子量

395.46

性状

固体

Formula

C23H21N7
CAS 号
运输条件

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

纯度 & 产品资料
参考文献

GW2974 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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:

GW2974202272-68-2GW 2974GW-2974EGFREpidermal growth factor receptorErbB-1HER1HER2glioblastomaInhibitorinhibitorinhibit

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