ARV-471 (Synonyms: ARV-471) |
| カタログ番号GC62723 |
ARV-471 は、乳癌に対する経口エストロゲン受容体 PROTAC タンパク質分解剤です。 ARV-471 は、エストロゲン受容体アルファと細胞内 E3 リガーゼ複合体の間の相互作用を促進するヘテロ二官能性分子です。 ARV-471は、プロテアソームを介してエストロゲン受容体のユビキチン化とそれに続く分解を引き起こします。 ARV-471 は、ER 陽性乳癌細胞株の ER を、最大分解濃度の半分 (DC50) ～ 2 nM で確実に分解します。
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Cas No.: 2229711-68-4
Sample solution is provided at 25 µL, 10mM.
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ARV-471 is an orally bioavailable estrogen receptor-targeted (ER-targeted) PROTAC for the treatment of patients with locally advanced or metastatic ER+/HER2- breast cancer[1].
ARV-471 induces degradation of wild-type and mutant ER (≥90%), including MCF-7 cells and ESR1 mutant lines[1]. ARV-471 can inhibit the proliferation of MCF7, T47D, T47D ER-Y537S and T47D ER-D538G cells, with GI50 of 3.3, 4.5, 7.9 and 5.7 nM, respectively[2].
ARV-471 (10 and 30 mpk, 27 days) can inhibit the growth of Patient-Derived tumor Xenograft model with ESR1 mutations and has a good tumor inhibitory effect[1]. ARV-471 (3, 10 and 30 mg/kg, 28 days) dose-dependently inhibited tumor growth in the MCF7 orthotopic xenograft model and promoted ER degradation (≥94%)[2].
References:
[1] Snyder L B, Flanagan J J, Qian Y, et al. The discovery of ARV-471, an orally bioavailable estrogen receptor degrading PROTAC for the treatment of patients with breast cancer[J]. Cancer Res, 2021, 81(13): 44.
[2] Gough S M, Flanagan J J, Teh J, et al. Oral estrogen receptor PROTAC® vepdegestrant (ARV-471) is highly efficacious as monotherapy and in combination with CDK4/6 or PI3K/mTOR pathway inhibitors in preclinical ER+ breast cancer models[J]. Clinical Cancer Research, 2024.
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