Mobocertinib

Research use only, not for human use.

Mobocertinib is a potent inhibitor of epidermal growth factor receptor (EGFR) and an antineoplastic agent.

Mobocertinib is a potent inhibitor of epidermal growth factor receptor (EGFR) and an antineoplastic agent.(In Vitro):Mobocertinib (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC50 of 21 nM.Mobocertinib (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 (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells.Mobocertinib (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling.Mobocertinib (0.01, 0.1 and 1 μM; 6 h) inhibits HER2 signaling in H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells.(In Vivo):Mobocertinib (3, 10, 30 mg/kg; p.o.; once daily for 20 days) significantly induces tumor growth inhibition.

Mobocertinib (1.5 nM-10 μM; 7 days) inhibits LU0387 (NPH) cells with IC50 of 21 nM.Mobocertinib (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 (0.1 nM-1 μM; 6 h) inhibits pEGFR and pERK1/2 in CUTO14 (ASV) cells.Mobocertinib (0.3 nM-1 μM; 6 h) inhibits EGFR and downstream signaling.Mobocertinib (0.01, 0.1 and 1 μM; 6 h) inhibits HER2 signaling in H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells.Cell Viability AssayCell Line:LU0387 (NPH) cells Concentration:1.5 nM-10 μM Incubation Time:7 days Result:Showed good inhibition activity for LU0387 (NPH) cells with IC50 of 21 nM.Cell Viability Assay Cell Line:A431 (WT), HCC827 (D), HCC4011 (L), H1975 (LT) cells Concentration:Incubation Time:2 hResult: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); IC50 of 35 nM).Western Blot Analysis 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 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 Cell Line:H1781 (HER2 Exon 20G776>VC), Ba/F3 (HER2 exon 20YVMA) cells Concentration:0.01, 0.1 and 1 μMIncubation Time:6 h Result:Inhibited HER2 signaling in H1781 and Ba/F3-HER2 exon 20YVMA mutant cells at 0.1 μM with significantly decreased phosphorylations of HER2, AKT, and ERK1/2 in a dose-dependent manner.

Mobocertinib (3, 10, 30 mg/kg; p.o.; once daily for 20 days) significantly induces tumor growth inhibition. 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.

tak788

Angiogenesis

EGFR

EGFR

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1847461-43-1

585.71

C32H39N7O4?

>98% (HPLC)

In Vitro:?DMSO : 25 mg/mL (42.68 mM)

COc1cc(N(C)CCN(C)C)c(NC(=O)C=C)cc1Nc1ncc(C(=O)OC(C)C)c(n1)-c1cn(C)c2ccccc12

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(-20℃)

With Ice Pack

≥ 2 years