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Larotrectinib (LOXO-101 free base)

产品编号: DC22338 Featured
Larotrectinib (LOXO-101 free base)
结构式
1223403-58-4
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中国地区超过5000个高品质化合物库存
应用领域
Larotrectinib (LOXO-101) 是一种 ATP 竞争性的、口服选择性抑制剂，对原肌凝蛋白相关激酶 (TRK) 家族受体的三个亚型 (TRKA，B 和C) 具有纳摩尔级别的 50% 抑制浓度。
化学性质生物活性化合物的使用COA & MSDS相关产品产品说明书
Cas No.: 1223403-58-4
名称:
别名: LOXO101,LOXO 101
SMILES: O=C(N1CC[C@@H](C1)O)NC2=C3N=C(N4CCC[C@@H]4C5=CC(F)=CC=C5F)C=CN3N=C2
分子式: C21H22F2N6O2
分子量: 428.17
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases. in vitro: LOXO-101 is an orally administered inhibitor of the TRK kinase and is highly selective only for the TRK family of receptors. LOXO-101 is evaluated for off-target kinase enzyme inhibition against a panel of 226 non-TRK kinases at a compound concentration of 1,000 nM and ATP concentrations near the Km for each enzyme. In the panel, LOXO-101 demonstrates greater than 50% inhibition for only one non-TRK kinase (TNK2 IC50, 576 nM). Measurement of proliferation following treatment with LOXO-101 demonstrates a dose-dependent inhibition of cell proliferation in all three cell lines. The IC50 is less than 100 nM for CUTO-3.29 and less than 10 nM for KM12 and MO-91, consistent with the known potency of this drug for the TRK kinase family. LOXO-101 demonstrates potent and highly-selective inhibition of TRKA, TRKB, and TRKC over other kinase- and non-kinase targets. LOXO-101 is a potent, ATP-competitive TRK inhibitor with IC50s in low nanomolar range for inhibition of all TRK family members in binding and cellular assays, with 100x selectivity over other kinases. in vivo: Athymic nude mice injected with KM12 cells are treated with LOXO-101 orally daily for 2 weeks. Dose-dependent tumor inhibition is observed, demonstrating the ability of this selective compound to inhibit tumor growth in vivo.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
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MSDS_1154_DC22338_1223403-58-4
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