2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. TAS2940 fumarate

TAS2940 fumarate 是一种可穿透大脑、具有口服活性、不可逆且具有选择性的泛 ERBB 抑制剂。TAS2940 fumarate 对野生型 HER2、HER2 V777L 和 A775_G776insYVMA 的 IC50 值分别为 5.6 nM、2.1 nM 和 1.0 nM。TAS2940 fumarate 可用于研究具有 HER2 和 EGFR 异常的肿瘤。

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TAS2940 fumarate Chemical Structure

TAS2940 fumarate Chemical Structure

CAS No. : 2758034-98-7

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Other Forms of TAS2940 fumarate:

TAS2940 fumarate 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

TAS2940 fumarate is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 fumarate against wild-type HER2, HER2 V777L, and A775_G776insYVMA with IC50 values of 5.6 nM, 2.1 nM, and 1.0 nM, respectively. TAS2940 fumarate can be used for the study of tumors with HER2 and EGFR aberrations[1].

体外研究
(In Vitro)

TAS2940 fumarate (10-100 nM；3-48 小时) 显著增加 B 细胞淋巴瘤 2 相互作用的细胞死亡介质 (BIM) 和裂解 PARP 的蛋白水平。TAS2940 fumarate 抑制 HER2、HER3 及其下游蛋白 AKT 和 ERK的磷酸化[1] 。
TAS2940 fumarate 抑制 MCF10A_HER2、MCF10A_HER2/S310F、MCF10A_HER2/L755S、MCF10A_HER2/V777L、MCF10A_HER2/V842I、MCF10A_HER2/insYVMA、MCF10A_EGFR、MCF10A_EGFR (EGF+)、MCF10A_EGFR/V769_D770insASV 和 MCF10A_EGFR/D770_N771insSVD 细胞，IC50 值分别为 2.27 nM、1.98 nM、3.74 nM、1.54 nM、3.28 nM、1.91 nM、9.38 nM、0.804 nM， 5.64 nM 和 2.98 nM[1]。

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

TAS2940 fumarate 相关抗体:

Western Blot Analysis[1]

Cell Line: SK-BR-3 cells
Concentration: 10 nM, 30 nM, 100 nM
Incubation Time: 3 h and 48 h
Result: Inhibited the phosphorylation of HER2, HER3, AKT, and ERK.
体内研究
(In Vivo)

TAS2940 fumarate（3.1-25 mg/kg；口服；每日一次；持续 14 天）可抑制具有 ERBB 畸变的异种移植小鼠模型中的肿瘤生长：HER2 扩增、HER2/EGFR 外显子 20 插入和 EGFR vIII 突变[1]。
雄性 BALB/cAJcl-nu/nu 小鼠单次口服或多次口服 7 天后 TAS2940 的 PK 参数[1]。
1.19

Administration Dose (mg/kg) Tmax (h) Apparent T1/2 (h) Cmax (ng/mL) AUClast (ng▪h/mL)
Single administration 6.25 0.33±0.14 2.15±2.15 601±111 795±229
Single administration 12.5 0.25±0.00 NC 1590±220 2010±230
Single administration 25 0.25±0.00 2.09 3580±190 5080±820
Repeated administrations for 7 days 6.25 0.25±0.00 2.20±2.73 1170±300 972±239
Repeated administrations for 7 days 12.5 0.33±0.14 0.69 2040±230 2800±460
Repeated administrations for 7 days 25 0.42±0.14 0.76 3710±360 6180±310

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

Animal Model: 6-week-old male BALB/cAJcl-nu/nu mice injected with NCI-N87, MCF10A_HER2/insYVMA_v, or NCI-H1975 EGFR D770_N771insSVD cellsMCF10A_HER2/insYVMA_v[1]
Dosage: 3.1-25 mg/kg (0.5 w/v% HPMC)
Administration: po; once daily; for 14 days
Result: Inhibited tumor growth in xenograft mouse models.
分子量

598.65

Formula

C32H34N6O6
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

TAS2940 fumarate 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:

TAS29402758034-98-7TAS 2940TAS-2940EGFREpidermal growth factor receptorErbB-1HER1ERBB inhibitorbrain-penetrableirreversibletumors with HER2 and EGFR aberrationsInhibitorinhibitorinhibit

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