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Selitrectinib (LOXO-195) 是异种选择性的二代原肌凝蛋白相关激酶(TRK)抑制剂,能够作用于 TRKA (IC50:0.6 nM) 和 TRKC (IC50<2.5 nM)。
Selitrectinib (LOXO-195) 是异种选择性的二代原肌凝蛋白相关激酶(TRK)抑制剂,能够作用于 TRKA (IC50:0.6 nM) 和 TRKC (IC50<2.5 nM)。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 347 | 现货 | |
5 mg | ¥ 798 | 现货 | |
10 mg | ¥ 1,220 | 现货 | |
25 mg | ¥ 2,380 | 现货 | |
50 mg | ¥ 3,560 | 现货 | |
100 mg | ¥ 4,760 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 892 | 现货 |
产品描述 | 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). |
靶点活性 | TrkA:0.6 nM , TrkC:<2.5 nM |
体内活性 | 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. |
动物实验 | 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. |
别名 | LOXO-195 |
分子量 | 380.42 |
分子式 | C20H21FN6O |
CAS No. | 2097002-61-2 |
Smiles | [H][C@]12CCCN1c1ccn3ncc(C(=O)N[C@H](C)CCc4ncc(F)cc24)c3n1 |
密度 | 1.51 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
溶解度信息 | DMSO: 65 mg/mL (170.86 mM) | |||||||||||||||||||||||||||||||||||
溶液配制表 | ||||||||||||||||||||||||||||||||||||
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