2. Metabolic Enzyme/Protease
  3. Tyrosine Hydroxylase
  4. GW583340

GW583340 (compound 6) 是一种 ErbB-2/EGFR 酪氨酸激酶抑制剂，具有口服活性。GW583340 在 EGFR 过表达和 ErbB-2 过表达的异种移植模型中表现出抗肿瘤活性。GW583340 可用于头颈癌、乳腺癌、胃癌的相关研究。

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GW583340

GW583340 Chemical Structure

CAS No. : 388082-81-3

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GW583340 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GW583340 (compound 6) is an orally active ErbB-2/EGFR tyrosine kinase inhibitor. GW583340 exhibits antitumor activity in xenograft models with EGFR overexpression or ErbB-2 overexpression. GW583340 is applicable to research related to head and neck cancer, breast cancer, and gastric cancer[1].

体外研究
(In Vitro)

GW583340 (compound 6) 可在体外无细胞实验中强效抑制纯化的 EGFR 和 ErbB-2 酪氨酸激酶活性，其双酶抑制的平均 IC50 为 0.012 μM[1]。
GW583340 (compound 6) 可强效且选择性地抑制 EGFR 过表达的 HN5、ErbB-2 过表达的 N87 以及 ErbB-2 过表达的 BT474 人肿瘤细胞系的增殖，其肿瘤细胞平均 IC50 为 0.11 μM，肿瘤细胞相对于正常 HFF 细胞的选择性比率>210 倍[1]。

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

GW583340 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Bioavailability
Mice[1] 10 mg/kg p.o. 39.5 %
体内研究
(In Vivo)

GW583340 (compound 6) (灌胃，每日 2 次，连续 21 天，剂量 30-100 mg/kg) 可在雌性 CD-1 小鼠的 HN5 EGFR 过表达人头颈癌异种移植模型中产生 81% 的肿瘤抑制率[1]。
GW583340 (灌胃，每日 2 次，连续 21 天，剂量 30-100 mg/kg) 可在雌性 CD-1 小鼠的 BT474 ErbB-2 过表达人乳腺癌异种移植物中产生 83%的肿瘤抑制率，且未观察到显著的体重下降[1]。

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

Animal Model: CD-1 (female)[1]
Dosage: 30 mg/kg; 100 mg/kg
Administration: p.o.; twice daily; 21 days
Result: Produced 81% tumor inhibition at 100 mg/kg.
Produced a lower level of tumor inhibition relative to the 100 mg/kg dose at 30 mg/kg.\nProduced 83% tumor inhibition at 100 mg/kg.
Produced a lower level of tumor inhibition relative to the 100 mg/kg dose at 30 mg/kg.
Showed no significant body weight loss in treated mice, indicating a good therapeutic index.
分子量

598.11

Formula

C28H25ClFN5O3S2
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

GW583340 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

GW583340388082-81-3GW 583340GW-583340Tyrosine HydroxylaseTyrH, THxenograft modelsHN5N87ErbB-2gastric carcinomatyrosine kinasehead and neck carcinomaEGFRnormal human foreskin fibroblastsbreast carcinomaInhibitorinhibitorinhibit

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