Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AV-412 free base is an EGFR inhibitor (IC50s: 0.75, 0.79, 0.5, 2.3, 19 nM for EGFR, EGFR(T790M), EGFR(L858R), EGFR(L858R/T790M) and ErbB2).
ターゲット&IC50 | EGFR:0.75 nM, EGFR (L858R):0.51 nM, EGFR (T790M):0.79 nM, EGFR (L858R/T790M):2.3 nM, ErbB2:19 nM |
In vivo | In cancer xenograft models, AV-412 (30 mg/kg) effectively halts the growth of A431 and BT-474 cell lines, which notably overexpress EGFR and ErbB2, respectively. This compound also inhibits autophosphorylation of EGFR and ErbB2, correlating with its antitumor properties. AV-412 exhibits considerable antitumor activity across different dosing regimens, displaying significant efficacy with daily and every-other-day administrations, but not with once-weekly dosing. Additionally, it significantly combats the gefitinib-resistant, ErbB2-overexpressing breast cancer cell line KPL-4, affirming its potent antitumor effects. |
別名 | MP-412 free base |
分子量 | 507 |
分子式 | C27H28ClFN6O |
CAS No. | 451492-95-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 48 mg/mL (94.68 mM)
You can also refer to dose conversion for different animals. 詳細
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AV-412 free base 451492-95-8 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR MP 412 AV 412 AV412 free base AV 412 free base MP-412 MP-412 free base MP412 AV-412 AV412 Inhibitor inhibitor inhibit