Larotrectinib (LOXO-101) sulfate

For research use only. Not for use in humans.

目录号：S7960 别名： ARRY-470, Larotrectinib

Larotrectinib (LOXO-101) sulfate Chemical Structure

CAS No. 1223405-08-0

Larotrectinib (LOXO-101) sulfate 是一种可口服的、选择性的、ATP竞争性的原肌球蛋白受体激酶TRK的有效抑制剂。Larotrectinib 对TRKs的抑制作用可诱导细胞凋亡和G1细胞周期阻滞。

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客户使用Selleck生产的Larotrectinib (LOXO-101) sulfate发表文献9篇：

客户使用该产品的3个实验数据：

  • Quantification of colony formation in (A), shown as a percentage of the control for NCIH2077 and RT112. Mean (3 biological replicates) +/- standard deviation (SD) shown (* p-value < 0.05, ** < 0.005, *** < 0.0005, two-sided t-test, comparing combination treatment to BGJ398 treatment). ns = not significant. (BGJ, BGJ398; Tram, Trametinib; BKM, BKM120; AZD, 8931; LDC, LDC1267; LOXO, LOXO-101; Imat, Imatinib; MGCD, MGCG-265).

    molecular cancer therapeutics. Larotrectinib (LOXO-101) sulfate purchased from Selleck.

    Immunoblot analysis for FRS2, AKT, and ERK activity for NCI-H2077 cells treated for 48 hours with DMSO, BGJ398, or additional kinase inhibitors as indicated, or combination treatment as indicated (Tram, trametinib; LDC, LDC1267; LOXO, LOXO-101; Imat, imatinib; MGCD, MGCG-265).

    Mol Cancer Ther, 2018, 17(7):1526-1539. Larotrectinib (LOXO-101) sulfate purchased from Selleck.

  • Inhibition of TRKA phosphorylation by Larotrectinib in NGF stimulated HEK293 cells. X-axis denotes concentrations of larotrectinib in nM. Y-Axis denotes percent inhibition of TRKA phosphorylation. Average IC50 of larotrectinib was found to be 10.9 nM. NGF: Neurite growth factor.

    Analytical Biochemistry, 2018, 545(15):78-83. Larotrectinib (LOXO-101) sulfate purchased from Selleck.

产品安全说明书

Trk receptor抑制剂选择性比较

生物活性

产品描述 Larotrectinib (LOXO-101) sulfate 是一种可口服的、选择性的、ATP竞争性的原肌球蛋白受体激酶TRK的有效抑制剂。Larotrectinib 对TRKs的抑制作用可诱导细胞凋亡和G1细胞周期阻滞。
靶点
TRK [1]
()
体外研究

ARRY-470(LOXO-101)是一种选择性的激酶抑制剂，对TRKA、TRKB和TRKC具有摩尔级别的活性，而对其他激酶的抑制活性都大于1000 nM。ARRY-470并不对表达其他致癌基因（上皮生长因子受体EGFR、ALK或ROS1）的Ba/F3细胞具有增殖抑制的作用、对来自于肺和结肠的不具有NTRK1融合的细胞系也没有此作用。ARRY-470(LOXO-101)能诱导KM12细胞的凋亡并将细胞周期阻滞在G1期[2]。
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
KM12 cells M{\iNmZ2dmO2aX;uJIF{e2G7 M3\KS|AtKDFyLDCxNFAtKDFyMECgcm0> MkjjN{Bpd3W{cx?= NH\MR3pNV1iRLUGwNUBqdmirYnn0[YQhVlSUS{GgdIhwe3Cqb4L5cIF1cW:wIHH0JFExOCCwbX;sM2w> Mm\GNlg4PTF3M{m=
Ba/F3 M1fxSWZ2dmO2aX;uJIF{e2G7 M{LxbVAtKDFyLDCxNFAtKDFyMECgcm0> NF3VV|c{KGixdYLz MmnsUG9ZVy1zMEGgbY5pcWKrdHXkJG5VWktzIIDoc5NxcG:{eXzheIlwdiCjdDCxNFAhdm2xbD;MMC=> NIj2VG0zQDd3MUWzPS=>
CR20 Ml;NSpVv[3Srb36gZZN{[Xl? M{XIZlAtKDFyLDCxNFAtKDFyMECgcm0> NWLDNY95OyCqb4Xydy=> NUXVdZZWVlSUS{GgdIhwe3Cqb4L5cIF1cW:wIIfhd{BqdmirYnn0[YQ> MVeyPFc2OTV|OR?=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-NTRK(Y490) / p-ERK (T202/Y204) / p-Eif4e; 

PubMed: 29568395     


Western blots of KM-12 cells treated with merestinib, crizotinib, entrectinib and larotrectinib in vitro. Cells were treated with compound ranging from 3.9 - 1000 nM for 2 hours. Western blots were re-probed for total NTRK, ERK, eIF4E and β-actin for loading control purposes.

pTRKA / TRKA / pTRKC / TRKC / p-AKT / AKT; 

PubMed: 26216294     


(E) LOXO-101 inhibits phosphorylation of Y496 of TPM3-TRKA kinase and downstream phosphorylation of ERK1/2 and S473 AKT in KM12 cells. (F) LOXO-101 inhibits phosphorylation of TEL-TRKC kinase and ERK1/2 and AKT phosphorylation in MO-91 cells. Cells were treated for 2 hours with the indicated doses of LOXO-101 or DMSO alone and cell lysates were analyzed using the indicated antibodies except for MO-91 cells were treated for 2 hours with 100 nM of LOXO-101 or DMSO alone and cell lysates were immunoprecipitated with an anti-TRK antibody followed by immunoblot analysis with the indicated antibodies. 

29568395 26216294
Growth inhibition assay
Cell proliferation; 

PubMed: 26216294     


(A)–(C) Dose-dependent inhibition with LOXO-101 is demonstrated in three cancer cell line models of oncogenic TRK. CUTO-3.29 lung adenocarcinoma with MPRIP-NTRK1 (A), KM12 colorectal cancer with TPM3-NTRK1(B), and MO-91 acute myeloid leukemia with ETV6-NTRK3 (C) cell lines were treated with a dose range of LOXO-101 and cellular proliferation was assayed by MTS assay. The cellular was IC50 was ~59.4 ± 2.2 nM for CUTO-3.29, 3.5 ± 0.7 nM for KM12 and 1.0 ± 0.05 nM for MO-91.

26216294
体内研究 早期持续的ARRY-470(LOXO-101) 的给药在荷瘤骨中能够显著地减弱骨癌疼痛、抑制感觉神经纤维的异位发芽以及类似神经瘤的结构的形成。但对肿瘤生长和骨骼重建没有显著效果。ARRY-470(LOXO-101)跨越血脑屏障的能力非常有限[1]。

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验：[2]
- 合并
  • Cell lines: Ba/F3细胞
  • Concentrations: 10, 100, 1000 nM
  • Incubation Time: 5 h
  • Method: 表达MPRIP-NTRK1 (RIP-TRKA)或EV的Ba/F3细胞用药物（DMSO；ARRY-470； G, gefitinib 1,000 nM）处理5小时后进行裂解，然后进行Werstern blot分析。
    (Only for Reference)
动物实验：[1]
- 合并
  • Animal Models: C3H/HeJ成年雄性小鼠
  • Dosages: 10-100 mg/kg
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (189.92 mM)
Water Insoluble
Ethanol '100 mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 526.51
化学式

C21H22F2N6O2.H2SO4
CAS号 1223405-08-0
储存条件 粉状
溶于溶剂
别名 ARRY-470, Larotrectinib

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、MSDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04142437 Recruiting Drug: larotrectinib(Vitrakvi BAY2757556) Locally Advanced or Metastatic Solid Tumor Harboring an NTRK Gene Fusion Bayer April 3 2020 --
NCT03834961 Recruiting Drug: Larotrectinib Sulfate Central Nervous System Neoplasm|Infantile Fibrosarcoma|Recurrent Acute Leukemia|Refractory Acute Leukemia|Solid Neoplasm Children''s Oncology Group|National Cancer Institute (NCI) September 18 2019 Phase 2
NCT02637687 Recruiting Drug: Larotrectinib (Vitravki BAY2757556) Solid Tumors Harboring NTRK Fusion Bayer December 16 2015 Phase 1|Phase 2
NCT02576431 Recruiting Drug: BAY2757556 (Larotrectinib Vitrakvi) Solid Tumors Harboring NTRK Fusion Bayer September 30 2015 Phase 2
NCT02122913 Active not recruiting Drug: Larotrectinib (Vitrakvi BAY2757556) Solid Tumors Harboring NTRK Fusion Bayer May 4 2014 Phase 1

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Trk receptor Signaling Pathway Map
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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID