Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Selitrectinib (LOXO-195) is a potent and selective inhibitor of the receptor tyrosine kinases(TRK)( TrkA and TrkC with IC50s of 0.6 and <2.5 nM, respectively)
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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1 mg | 在庫あり | ¥ 8,000 | |||
5 mg | 在庫あり | ¥ 18,500 | |||
10 mg | 在庫あり | ¥ 28,000 | |||
25 mg | 在庫あり | ¥ 55,000 | |||
50 mg | 在庫あり | ¥ 81,500 | |||
100 mg | 在庫あり | ¥ 108,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 19,500 |
説明 | Selitrectinib (LOXO-195) is a potent and selective inhibitor of the receptor tyrosine kinases(TRK)( TrkA and TrkC with IC50s of 0.6 and <2.5 nM, respectively) |
ターゲット&IC50 | TrkA:0.6 nM , TrkC:<2.5 nM |
In vivo | Selitrectinib (≥30 mg/kg) reduces tumor growth in TrkA-dependent KM12, as well as NIH 3T3 ΔTrkA, ΔTrkA + TrkAG595R, and ΔTrkA + TrkAG667C mouse xenograft models. |
動物実験 | Each cell line (2–5×10e6 cells) was injected subcutaneously into female nu/nu NCr mice age 7–9 weeks and allowed to grow to ~100–200 mm3 (efficacy) or ~ 500mm3 (PK-PD) prior to randomization by tumor size and treatment with each inhibitor by oral gavage.?For PK-PD analysis, animals were dosed for 3 days, followed by euthanasia, excision of tumors and collection of plasma.?Phospho-TRK levels in tumor lysates were determined by ELISA assay, while plasma inhibitor levels were determined by LC-MS/MS.?For efficacy analysis, animals were dosed by oral gavage, and body weight and tumor size were monitored at regular intervals. |
別名 | LOXO-195 |
分子量 | 380.42 |
分子式 | C20H21FN6O |
CAS No. | 2097002-61-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 62.5 mg/mL (164.29 mM)
You can also refer to dose conversion for different animals. 詳細
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Selitrectinib 2097002-61-2 Tyrosine Kinase/Adaptors Trk receptor LOXO195 Inhibitor LOXO 195 Tropomyosin related kinase receptor LOXO-195 Trk Receptor inhibit inhibitor