(S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolid
CAS号 1223405-08-0 SDF Download SDF
化学名 (S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolidine-1-carboxamide sulfate
SMILES O=S(O)(O)=O.O=C(N1C[C@@H](O)CC1)NC2=C3N=C(N4[C@@H](C5=CC(F)=CC=C5F)CCC4)C=CN3N=C2
分子式 C21H24F2N6O6S 分子量 526.51
溶解性 Soluble in DMSO 储存条件 Store at -20°C
一般建议 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。
(3S)-N-[5-[(2R)-2-(2,5-二氟苯基)-1-吡咯烷基]吡唑并[1,5-a]嘧啶-3-基]-3-羟基-1-吡咯烷甲酰胺硫酸盐
商品名称
CAS号 1223405-08-0
分子式 C21H24F2N6O6S
分子量 526.51400
LogP 3.45140
PSA 168.98000
产品描述: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. ic50 value: 2 - 20 nm target: trka/b/c 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. [1] 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. [2] 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.
![(S)-N-(5-((R)-2-(2,5-difluorophenyl)pyrrolidin-1-yl)pyrazolo[1,5-a]pyrimidin-3-yl)-3-hydroxypyrrolid](https://cimg.cphi.cn/img_Cphi_cn/Product/2018_06/Mimg_1806250405575253.jpg)
![(3S)-N-[5-[(2R)-2-(2,5-二氟苯基)-1-吡咯烷基]吡唑并[1,5-a]嘧啶-3-基]-3-羟基-1-吡咯烷甲酰胺硫酸盐](https://cimg.cphi.cn/img_Cphi_cn/Product/2018_03/Mimg_1803120237510206.jpg)
