AV-412 (MP412) 是 EGFR 抑制剂，抑制EGFR，EGFR^L858R，EGFR^T790M，EGFR^L858R/T790M 和 ErbB2的 IC₅₀ 值分别为0.75，0.5，0.79，2.3，19 nM。

AV-412 (MP412) is an EGFR inhibitor with IC 50 s of 0.75, 0.5, 0.79, 2.3, 19 nM for EGFR, EGFR, EGFR, EGFR and ErbB2, respectively.

Solid

EGFR 0.75 nM (IC50) EGFR 0.5 nM (IC50

AV-412 inhibits autophosphorylation of EGFR and ErbB2 with IC50 of 43 and 282 nM, respectively. AV-412 also inhibits epidermal growth factor (EGF)-dependent cell proliferation with an IC50 of 100 nM. AV-412 abrogates EGFR signaling in the gefitinib-resistant H1975 cell line, which harbors a double mutation of L858R and T790M in EGFR. has not independently confirmed the accuracy of these methods. They are for reference only.

In animal studies using cancer xenograft models, AV-412 (30 mg/kg) demonstrates complete inhibition of tumor growth of the A431 and BT-474 cell lines, which overexpress EGFR and ErbB2, respectively. AV-412 suppresses autophosphorylation of EGFR and ErbB2 at the dose corresponding to its antitumor efficacy. When various dosing schedules are applied, AV-412 shows 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, AV-412 shows a significant antitumor effect on the ErbB2-overexpressing breast cancer KPL-4 cell line, which is resistant to gefitinib. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

[1]. Suzuki T, et al. Pharmacological characterization of MP-412 (AV-412), a dual epidermal growth factor receptorand ErbB2 tyrosine kinase inhibitor. Cancer Sci. 2007 Dec;98(12):1977-84.

In Vitro: DMSO : ≥ 28 mg/mL (32.89 mM)配制储备液