Powder: -20°C for 3 years | In solvent: -80°C for 1 year
AV-412 (MP412) is an EGFR inhibitor (EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M and ErbB2 with IC50s of 0.75, 0.79, 0.5, 2.3, 19 nM).
説明 | AV-412 (MP412) is an EGFR inhibitor (EGFR, EGFR T790M, EGFR L858R, EGFR L858R/T790M and ErbB2 with IC50s of 0.75, 0.79, 0.5, 2.3, 19 nM). |
ターゲット&IC50 | EGFR (L858R):0.5 nM, EGFR:0.75 nM, EGFR (T790M):0.79 nM, ErbB2:19 nM, EGFR (L858R/T790M):2.3 nM |
In vitro | In cells, MP-412 inhibited autophosphorylation of EGFR and ErbB2 with IC(50) of 43 and 282 nM, respectively. It also inhibited epidermal growth factor (EGF)-dependent cell proliferation with an IC(50) of 100 nM. Moreover, MP-412 abrogated EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. |
In vivo | In animal studies using cancer xenograft models, MP-412 (30 mg/kg) demonstrated complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively.MP-412 suppressed autophosphorylation of EGFR and ErbB2 at the dose corresponding to its antitumor efficacy.When various dosing schedules were applied, MP-412 showed significant effects with daily and every-other-day schedules, but not with a once-weekly schedule, suggesting that frequent dosing is preferable for this compound.Furthermore, MP-412 showed a significant antitumor effect on the ErbB2-overexpressing breast cancer KPL-4 cell line, which is resistant to gefitinib.These studies indicate that MP-412 has potential as a therapeutic agent for the treatment of cancers expressing EGFR and ErbB2, especially those resistant to the first generation of small-molecule inhibitors. |
別名 | MP412 |
分子量 | 851.41 |
分子式 | C41H44ClFN6O7S2 |
CAS No. | 451493-31-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 25 mg/mL (29.36 mM)
You can also refer to dose conversion for different animals. 詳細
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AV-412 451493-31-5 Angiogenesis JAK/STAT signaling Tyrosine Kinase/Adaptors EGFR Inhibitor inhibit MP 412 HER1 Epidermal growth factor receptor AV412 MP412 AV 412 MP-412 ErbB-1 inhibitor