Mobocertinib (TAK-788) mesylate 是一种口服有效并且不可逆的EGFR/HER2抑制剂。Mobocertinib mesylate 能选择性地 (相较于野生型EGFR) 抑制含有EGFRex20ins的致癌突变体。Mobocertinib mesylate 可用于 NSCLC 的研究。
| 生物活性 | Mobocertinib (TAK-788) mesylate is an orally active and irreversibleEGFR/HER2inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activatingEGFRex20insmutations with selectivity over wild-typeEGFR. Mobocertinib mesylate can be used in NSCLC research[1][2]. |
| IC50& Target | HER2 | EGFR exon 20 insertion | EGFR (WT) |
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体外研究
(In Vitro) | Mobocertinib mesylate (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC50of 21 nM[1].
Mobocertinib mesylate (2 h) potently inhibits EGFR with common activating mutations (HCC827 (D), HCC4011 (L)) or with a T790M mutation (H1975 (LT)) more potently than WT EGFR (A431 (WT))[1].
Mobocertinib mesylate (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells[1].
Mobocertinib mesylate (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling[1].
Mobocertinib mesylate (0.01, 0.1 and 1 μM; 6 h) inhibits HER2 signaling in H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells[2].
Cell Viability Assay[1] | Cell Line: | LU0387 (NPH) cells | | Concentration: | 1.5 nM-10 μM | | Incubation Time: | 7 days | | Result: | Showed good inhibition activity for LU0387 (NPH) cells with IC50of 21 nM. |
Cell Viability Assay[1] | Cell Line: | A431 (WT), HCC827 (D), HCC4011 (L), H1975 (LT) cells | | Concentration: | | | Incubation Time: | 2 h | | Result: | Inhibited EGFR with common activating mutations of HCC827 (D), HCC4011 (L) cells and T790M mutation of H1975 (LT) with IC50s of 4, 1.3 and 9.8 nM respectively, which more potently than WT EGFR (A431 (WT); IC50of 35 nM). |
Western Blot Analysis[1] | Cell Line: | CUTO14 (ASV) cells | | Concentration: | 0.1 nM-1 μM | | Incubation Time: | 6 h | | Result: | Robustly inhibited EGFR signaling, reaching 80% and 100% inhibition of phosphorylated EGFR (pEGFR) at concentrations of 100 nM and 1 μM, respectively. |
Western Blot Analysis[1] | Cell Line: | HCC827 (D), HCC4011 (L), H1975 (LT) cells | | Concentration: | 0.3 nM-1 μM | | Incubation Time: | 6 h | | Result: | Potently inhibited EGFR and downstream signaling in HCC827 (D), HCC4011 (L) and H1975 (LT) cells. |
Western Blot Analysis[2] | Cell Line: | H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells | | Concentration: | 0.01, 0.1 and 1 μM | | Incubation Time: | 6 h | | Result: | Inhibited HER2 signaling in H1781 and Ba/F3-HER2 exon 20YVMAmutant cells at 0.1 μM with significantly decreased phosphorylations of HER2, AKT, and ERK1/2 in a dose-dependent manner. |
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体内研究
(In Vivo) | Mobocertinib mesylate (3, 10, 30 mg/kg; p.o.; once daily for 20 days) significantly induces tumor growth inhibition[1].
| Animal Model: | Animal model: Female Athymic Nude-Foxn1numice (human NSCLC H1975 LT tumor model)[1]. | | Dosage: | 3, 10, 30 mg/kg | | Administration: | Oral; once daily for 20 days. | | Result: | Decreased the mean tumor volume by 44% and 92% when at 3 mg/kg and 10 mg/kg, respectively, relative to the tumor size of vehicle group.
Induced a 76% tumor regression relative to the pretreatment tumor size at 30 mg/kg. |
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| 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. |
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