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受注：045-509-1970 |
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化学情報
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Synonyms | CS 3009, Gavreto | Storage (From the date of receipt) |
3 years -20°C powder |
| 化学式 | C27H32FN9O2 |
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| 分子量 | 533.60 | CAS No. | 2097132-94-8 | |
| Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (187.4 mM) | |
| Ethanol | 100 mg/mL (187.4 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | Pralsetinib (BLU-667, CS 3009, Gavreto) is a highly potent and selective RET (c-RET) inhibitor with an IC50 of 0.4 nM for WT RET. It also demonstrates potent activity (IC50 0.4 nmol/L) against common oncogenic RET alterations, including RET (M918T). |
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| in vitro | BLU-667 is at least 100-fold more selective for RET over 96% of kinases tested (a panel of 371 kinases). BLU-667 specifically abrogates RET signaling in RET-altered cancers from diverse lineages. RET pathway inhibition with BLU-667 also more potently inhibits proliferation of RET-altered cell lines relative to multikinase inhibitors[1]. |
| in vivo | In vivo, BLU-667 potently inhibits growth of NSCLC and thyroid cancer xenografts driven by various RET mutations and fusions without inhibiting VEGFR2. BLU-667 is well tolerated throughout the in vivo studies[1]. |
プロトコル(参考用のみ)
| キナーゼアッセイ | Human Kinase Selectivity | |
|---|---|---|
| BLU-667 is screened at 300 nmol/L for inhibitory activity across a panel of 371 kinases. The 23 kinases inhibited >50% at 300 nmol/L are selected for full 10 point concentration-response curves with BLU-667 (1 μmol/L maximum concentration) at 200 μmol/L ATP to generate biochemical IC50 (Reaction Biology Corp) using 33P-ATP (10 mCi/mL) to initiate the reaction, followed by the detection of kinase activity by a filter-binding method. | ||
| 細胞アッセイ | 細胞株 | LC2/ad cells, MZ-CRC-1 cells and TT cells |
| 濃度 | 0-1 μM | |
| 反応時間 | 90 minutes | |
| 実験の流れ | -- |
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| 動物実験 | 動物モデル | PDX tumor models (BALB/c nude mice) |
| 投薬量 | 3, 10, or 30 mg/kg twice daily or 60 mg/kg once daily | |
| 投与方法 | -- | |
Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：
| Lenvatinib enhances antitumor immunity by promoting the infiltration of TCF1+ CD8+ T cells in HCC via blocking VEGFR2 [ Cancer Sci, 2023, 114(4):1284-1296] | PubMed: 36609997 |
| Lenvatinib enhances antitumor immunity by promoting the infiltration of TCF1+ CD8+ T cells in HCC via blocking VEGFR2 [ Cancer Sci, 2023, 114(4):1284-1296] | PubMed: 36609997 |
| Loss of Tumour Suppressor TMEM127 Drives RET-mediated Transformation Through Disrupted Membrane Dynamics [ bioRxiv, 2023, 2023.06.28.546955] | PubMed: 37425958 |
| Novel Calcium-Binding Ablating Mutations Induce Constitutive RET Activity and Drive Tumorigenesis [ Cancer Res, 2022, 82(20):3751-3762] | PubMed: 36166639 |
| The kinase PLK1 promotes the development of Kras/Tp53-mutant lung adenocarcinoma through transcriptional activation of the receptor RET [ Sci Signal, 2022, 15(754):eabj4009] | PubMed: 36194647 |
| Targeting RET Kinase in Neuroendocrine Prostate Cancer [ Mol Cancer Res, 2020, 18(8):1176-1188] | PubMed: 32461304 |
| Elucidating the Mechanism of RET Kinase Activity in Neuroendocrine Prostate Cancer [ Mol Cancer Res, 2020, 1176-1188] | PubMed: None |
| Targeting RET Kinase in Neuroendocrine Prostate Cancer [ Mol Cancer Res, 2020, 27;molcanres.1245.2019] | PubMed: 32461304 |
| RET Kinase Signaling as a Key Switch Toward the Neuroendocrine Phenotype [ Defense Technical Information Center, 2020, N/A] | PubMed: N/A |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。