Amuvatinib

그림문자(GHS)

• 그림문자(GHS)

  

• 신호 어

  Warning

• 유해·위험 문구

  H315：피부에 자극을 일으킴

  H319：눈에 심한 자극을 일으킴

  H335：호흡 자극성을 일으킬 수 있음

• 예방조치문구

  P261：분진·흄·가스·미스트·증기·...·스프레이의 흡입을 피하시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P264：취급 후에는 손을 철저히 씻으시오.

  P271：옥외 또는 환기가 잘 되는 곳에서만 취급하시오.

  P280：보호장갑/보호의/보안경/안면보호구를 착용하시오.

  P302+P352：피부에 묻으면 다량의 물로 씻으시오.

  P304+P340：흡입하면 신선한 공기가 있는 곳으로 옮기고 호흡하기 쉬운 자세로 안정을 취하시오.

  P305+P351+P338：눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.

  P312：불편함을 느끼면 의료기관(의사)의 진찰을 받으시오.

  P321：(…) 처치를 하시오.

  P332+P313：피부 자극이 생기면 의학적인 조치· 조언을 구하시오.

  P337+P313：눈에 대한 자극이 지속되면 의학적인 조치· 조언를 구하시오.

  P403+P233：용기는 환기가 잘 되는 곳에 단단히 밀폐하여 저장하시오.

  P405：밀봉하여 저장하시오.

  P501：...에 내용물 / 용기를 폐기 하시오.

Amuvatinib 화학적 특성, 용도, 생산

• 개요

  Amuvatinib (also known as MP-470 or 850879-09-3), is a multi-targeted inhibitor of receptor tyrosine kinases that inhibits c-Kit, platelet-derived growth factor receptor α (PDGFRα), and c-Met (IC50s = 10, 40, and 81 nM, respectively). It inhibits growth and induces apoptosis in prostate cancer cell lines, with additive effects achieved when combined with erlotinib . Amuvatinib sensitizes cancer cells to radiation and chemotherapeutic compounds, in part by inhibiting homologous recombination.

• 용도

  MP-470 (Amuvatinib) is a potent and multi-targeted inhibitor of c-KitD816H, PDGFαV561D and Flt3D835Y with IC50 of 10 nM, 40 nM and 81 nM, respectively.

• Clinical Use

  Amivantamab is the first drug approved by the FDA for the treatment of patients with NSCLC and EGFR exon 20 insertion mutations.

• Mode of action

  Μechanisticly, amuvatinib inhibits tyrosine kinase receptor KIT through occupying its ATP binding domain (IC50 < 0.1 μM) and disrupts DNA repair through suppression of homologous recombination protein Rad51 as well as synergistic effects in combination with double stranded DNA damaging agents.

• 참고 문헌

  1. Effects of combining amuvatinib (MP-470) with DNA-damaging agents in osteosarcoma cell lines
  2. Janssen submits supplemental biologics license application to the U.S. Food and Drug Administration seeking approval of RYBREVANT? (amivantamab-vmjw) in combination with chemotherapy for the first-line treatment of patients with locally advanced or metastatic EGFR exon 20 insertion mutation-positive non-small cell lung cancer. News release.
  3. Raoul Tibes, Gil Fine, Gavin Choy, Sanjeev Redkar, Pietro Taverna, Aram Oganesian, Amarpao Sahai, Mohammad Azab and Anthony W. Tolcher. A phase I, first-in-human dose-escalation study of amuvatinib, a multi-targeted tyrosine kinase inhibitor, in patients with advanced solid tumors. Cancer Chemother Pharmacol (2013) 71: 463-471
  4. Gavin Choy, Rajashree Joshi-Hangal, Aram Oganesian, Gil Fine, Scott Rasmussen, Joanne Collier, James Kissling, Amarpal Sahai, Mohammad Azab and Sanjeev Redkar. Saftety, tolerability, and pharmacokinetics of amuvatinib from three phase 1 clinical studies in healthy volunteers. Cancer Chemother Pharmacol (2012) 70: 183-190

Amuvatinib 공급 업체

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