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

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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规格 价格 是否有货 数量
5 mg ￥1200
In-stock
10 mg ￥1950
In-stock
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100 mg   询价  

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Customer Review

GW2974 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

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

Formula

C23H21N7
CAS 号
性状

固体

颜色

Light yellow to yellow

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)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 20 mg/mL (50.57 mM; 超声加热助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5287 mL 12.6435 mL 25.2870 mL
5 mM 0.5057 mL 2.5287 mL 5.0574 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

GW2974 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5287 mL 12.6435 mL 25.2870 mL 63.2175 mL
5 mM 0.5057 mL 2.5287 mL 5.0574 mL 12.6435 mL
10 mM 0.2529 mL 1.2644 mL 2.5287 mL 6.3218 mL
15 mM 0.1686 mL 0.8429 mL 1.6858 mL 4.2145 mL
20 mM 0.1264 mL 0.6322 mL 1.2644 mL 3.1609 mL
25 mM 0.1011 mL 0.5057 mL 1.0115 mL 2.5287 mL
30 mM 0.0843 mL 0.4215 mL 0.8429 mL 2.1073 mL
40 mM 0.0632 mL 0.3161 mL 0.6322 mL 1.5804 mL
50 mM 0.0506 mL 0.2529 mL 0.5057 mL 1.2644 mL
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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目录号：
HY-112293
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