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编 号：F287733
分子式：C33H43N7O7S
分子量：681.8
分子式：C33H43N7O7S
分子量：681.8
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CAS No: 2389149-85-1
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Mobocertinib (TAK-788) mesylate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib mesylate can be used in NSCLC research.
体内研究：
Mobocertinib mesylate (3, 10, 30 mg/kg; p.o.; once daily for 20 days) significantly induces tumor growth inhibition.Animal Model:Animal model: Female Athymic Nude-Foxn1nu mice (human NSCLC H1975 LT tumor model).
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.
体外研究：
Mobocertinib mesylate (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC50 of 21 nM.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)).Mobocertinib mesylate (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells.Mobocertinib mesylate (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling.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.
Mobocertinib (TAK-788) mesylate is an orally active and irreversible EGFR/HER2 inhibitor. Mobocertinib mesylate potently inhibits oncogenic variants containing activating EGFRex20ins mutations with selectivity over wild-type EGFR. Mobocertinib mesylate can be used in NSCLC research.
体内研究：
Mobocertinib mesylate (3, 10, 30 mg/kg; p.o.; once daily for 20 days) significantly induces tumor growth inhibition.Animal Model:Animal model: Female Athymic Nude-Foxn1nu mice (human NSCLC H1975 LT tumor model).
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.
体外研究：
Mobocertinib mesylate (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC50 of 21 nM.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)).Mobocertinib mesylate (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells.Mobocertinib mesylate (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling.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.
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