Larotrectinib (LOXO-101) sulfate

For research use only. Not for use in humans.

目录号：S7960 别名： ARRY-470, Larotrectinib 中文名称：硫酸盐拉罗替尼

Larotrectinib (LOXO-101) sulfate Chemical Structure

CAS No. 1223405-08-0

Larotrectinib sulfate (LOXO-101, ARRY-470)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。

规格

价格

库存

购买数量

10mM (1mL in DMSO)	RMB 1449.63	现货
5mg	RMB 794.51	现货
25mg	RMB 2433.3	现货
100mg	RMB 6527.56	现货
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客户使用Selleck生产的Larotrectinib (LOXO-101) sulfate发表文献10篇：

Front Oncol, 2020, 12;10:700

PubMed: 32477943 ( click the link to review the publication )

Cancer Commun (Lond), 2020, 11

PubMed: 32525624 ( click the link to review the publication )

Cancers (Basel), 2020, 12(9):E2345

PubMed: 32825119 ( click the link to review the publication )

Cold Spring Harb Mol Case Stud, 2020, mcs.a005710

PubMed: 33144287 ( click the link to review the publication )

Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-3165

PubMed: 31871300 ( click the link to review the publication )

Cancers (Basel), 2019, 11(4)

PubMed: 30986992 ( click the link to review the publication )

Eur J Med Chem, 2019, 179:470-482

PubMed: 31271959 ( click the link to review the publication )

J Drug Target, 2019, 27(4):442-450

PubMed: 30301369 ( click the link to review the publication )

Mol Cancer Ther, 2018, 17(7):1526-1539

PubMed: 29654068 ( click the link to review the publication )

Anal Biochem, 2018, 545:78-83

PubMed: 29360440 ( click the link to review the publication )

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 sulfate (LOXO-101, ARRY-470)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	Activity Description	PMID
KM12 cells	Mm[wSpVv[3Srb36gZZN{[Xl?	NV\hcoxOOCxiMUCsJFExOCxiMUCwNEBvVQ>?	MoO3N{Bpd3W{cx?=	MnnwUG9ZVy1zMEGgbY5pcWKrdHXkJG5VWktzIIDoc5NxcG:{eXzheIlwdiCjdDCxNFAhdm2xbD;M	NWXtRndCOjh5NUG1N\|k>
Ba/F3	M{XoVGZ2dmO2aX;uJIF{e2G7	M4HwZlAtKDFyLDCxNFAtKDFyMECgcm0>	NX3WO4RROyCqb4Xydy=>	M1zQPGxQYE9vMUCxJIlvcGmkaYTl[EBPXFKNMTDwbI9{eGixconsZZRqd25iYYSgNVAxKG6vb3yvUEw>	MmPtNlg4PTF3M{m=
CR20	M2LvdmZ2dmO2aX;uJIF{e2G7	M1\z[FAtKDFyLDCxNFAtKDFyMECgcm0>	NF\UfHA{KGixdYLz	M3LKVW5VWktzIIDoc5NxcG:{eXzheIlwdiC5YYOgbY5pcWKrdHXk	NX7CXJZROjh5NUG1N\|k>

... 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 Oncotarget 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 Cancer Discov (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 Cancer Discov (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]。

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)

参考文献

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 Download Larotrectinib (LOXO-101) sulfate SDF

分子量	526.51
化学式	C₂₁H₂₂F₂N₆O₂.H₂SO₄
CAS号	1223405-08-0
储存条件	3年-20°C 粉状 2年-80°C 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

计算结果:

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL ddH₂O，混匀澄清。

注意：1. 首先保证母液是澄清的；
2. 一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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

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
初始浓度:
稀释倍数:

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

通过输入化合物的化学式来计算其分子量：

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 (data from https://clinicaltrials.gov, updated on 2020-01-06)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04655404	Not yet recruiting	Drug: Larotrectinib\|Procedure: Larotrectinib	High Grade Glioma	Nationwide Children''s Hospital	February 1 2021	Early Phase 1
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

研究领域

产品类型

定制您的化合物库

Larotrectinib (LOXO-101) sulfate

客户使用Selleck生产的Larotrectinib (LOXO-101) sulfate发表文献10篇：

客户使用该产品的3个实验数据：

产品安全说明书

Trk receptor抑制剂选择性比较

生物活性

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)

参考文献

溶解度 (25°C)

化学数据 Download Larotrectinib (LOXO-101) sulfate SDF

动物体内配方计算器 (澄清溶液)

计算器

摩尔浓度计算器

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

摩尔浓度计算公式

稀释计算器

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

连续稀释计算器方程

连续稀释

计算结果

分子量计算器

总分子量：g/mol

摩尔浓度计算器

临床试验信息 (data from https://clinicaltrials.gov, updated on 2020-01-06)

技术支持

Trk receptor Signaling Pathway Map