| Bioactivity | TAS2940 is a brain-penetrable, orally active, irreversible and selective pan-ERBB inhibitor. TAS2940 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 can be used for the study of tumors with HER2 and EGFR aberrations[1]. |
| Invitro | TAS2940 (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 抑制 HER2、HER3 及其下游蛋白 AKT 和 ERK的磷酸化[1] 。TAS2940 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. 0 --> TAS2940 相关抗体: |
| 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 |
| CAS | 2451398-65-3 |
| Formula | C28H30N6O2 |
| Molar Mass | 482.58 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Kei Oguchi, et al. TAS2940, a novel brain-penetrable pan-ERBB inhibitor, for tumors with HER2 and EGFR aberrations. Cancer Sci. 2023 Feb;114(2):654-664. |