Entrectinib

別名: RXDX-101, NMS-E628 中文名稱(chēng)：恩曲替尼

目錄號(hào)：S7998 Purity: 99.93%

Entrectinib是一種口服生物可利用的泛-TrkA/B/C，ROS1 和 ALK 抑制劑，IC50范圍為 0.1~1.7 nM。Entrectinib (RXDX-101) 可誘導(dǎo)自噬。Phase 2。

Entrectinib Chemical Structure

CAS: 1108743-60-7

規(guī)格	價(jià)格	庫(kù)存
10mM (1mL in DMSO)	1556.1	現(xiàn)貨
5mg	875.36	現(xiàn)貨
25mg	3073.41	現(xiàn)貨
100mg	6935.43	現(xiàn)貨
1g	12039.3	現(xiàn)貨
更大包裝有超大折扣
400-668-6834 [email protected]

產(chǎn)品質(zhì)控

批次：純度： 99.93%

99.93

Entrectinib相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	TrkA TrkB TrkC	點(diǎn)擊展開(kāi)
相關(guān)產(chǎn)品	ANA-12 GW441756 7,8-Dihydroxyflavone GNF-5837 Selitrectinib (LOXO-195) Altiratinib N-Acetyl-5-hydroxytryptamine	點(diǎn)擊展開(kāi)
相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) 酪氨酸激酶抑制劑分子庫(kù) PI3K/Akt 抑制劑庫(kù) 細(xì)胞周期化合物庫(kù) 血管生成相關(guān)化合物庫(kù)	點(diǎn)擊展開(kāi)

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類(lèi)型	給藥濃度	孵育時(shí)間	活性描述	文獻(xiàn)信息(PMID)
KARPAS299	Function assay	60 mg/kg	12 hrs	Ex vivo inhibition of NPM-ALK phosphorylation in SCID mouse xenografted with human KARPAS299 cells at 60 mg/kg, po administered as single dose measured after 12 hrs by Western blot analysis	27003761
KARPAS299	Function assay	60 mg/kg	18 hrs	Ex vivo inhibition of NPM-ALK phosphorylation in SCID mouse xenografted with human KARPAS299 cells at 60 mg/kg, po administered as single dose measured after 18 hrs by Western blot analysis	27003761
KARPAS299	Function assay	60 mg/kg	12 hrs	Ex vivo inhibition of NPM-ALK phosphorylation in SCID mouse xenografted with human KARPAS299 cells assessed as suppression of STAT3 phosphorylation at 60 mg/kg, po administered as single dose measured after 12 hrs by Western blot analysis	27003761
KARPAS299	Function assay	60 mg/kg	18 hrs	In vivo inhibition of NPM-ALK phosphorylation in SCID mouse xenografted with human KARPAS299 cells assessed as suppression of STAT3 phosphorylation at 60 mg/kg, po administered as single dose measured after 18 hrs by Western blot analysis	27003761
NCI-H2228	Antitumor assay	30 to 60 mg/kg	10 days	Antitumor activity against human NCI-H2228 cells xenografted in athymic nu/nu mouse assessed as tumor growth inhibition at 30 to 60 mg/kg, po bid administered for 10 days	27003761
NCI-H2228	Function assay	60 mg/kg	12 hrs	Ex vivo inhibition of EML4-ALK phosphorylation in athymic nu/nu mouse xenografted with human NCI-H2228 cells at 60 mg/kg, po administered as single dose measured after 12 hrs by Western blot analysis	27003761
NCI-H2228	Function assay	60 mg/kg	18 hrs	Ex vivo inhibition of EML4-ALK phosphorylation in athymic nu/nu mouse xenografted with human NCI-H2228 cells at 60 mg/kg, po administered as single dose measured after 18 hrs by Western blot analysis	27003761
NCI-H2228	Function assay	60 mg/kg	12 hrs	Ex vivo inhibition of EML4-ALK phosphorylation in athymic nu/nu mouse xenografted with human NCI-H2228 cells assessed as suppression of AKT phosphorylation at 60 mg/kg, po administered as single dose measured after 12 hrs by Western blot analysis	27003761
NCI-H2228	Function assay	60 mg/kg	18 hrs	Ex vivo inhibition of EML4-ALK phosphorylation in athymic nu/nu mouse xenografted with human NCI-H2228 cells assessed as suppression of AKT phosphorylation at 60 mg/kg, po administered as single dose measured after 18 hrs by Western blot analysis	27003761
KARPAS299	Antitumor assay	30 to 60 mg/kg	10 days	Antitumor activity against human KARPAS299 cells xenografted in SCID mouse assessed as tumor growth inhibition at 30 to 60 mg/kg, po bid administered for 10 days	27003761
KARPAS299	Antitumor assay	30 to 60 mg/kg	10 days	Antitumor activity against human KARPAS299 cells xenografted in SCID mouse assessed as tumor free cured mouse at 30 to 60 mg/kg, po bid administered for 10 days measured on day 90	27003761
BAF3	Function assay		72 hrs	Inhibition of human TEL (336 residues) fused-ROS1 (1891 to 2347 residues) (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.005 μM.	27003761
BAF3	Function assay		72 hrs	Inhibition of human TEL (336 residues) fused-TRKC (454 to 825 residues) (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.003 μM.	27003761
BAF3	Function assay		72 hrs	Inhibition of human TEL (336 residues) fused-TRKA (440 to 796 residues) (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.003 μM.	27003761
BAF3	Function assay		72 hrs	Inhibition of human TEL (336 residues) fused-TRKB (455 to 822 residues) (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.003 μM.	27003761
KM12	Antiproliferative assay		72 hrs	Antiproliferative activity against human KM12 cells expressing TRKA protein incubated for 72 hrs by cell titer-glo assay, IC50 = 0.017 μM.	27003761
SU-DHL1	Antiproliferative assay		72 hrs	Antiproliferative activity against human SU-DHL1 cells expressing ALK protein incubated for 72 hrs by cell titer-glo assay, IC50 = 0.024 μM.	27003761
BAF3	Function assay		72 hrs	Inhibition of wild type EML4-ALK (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.028 μM.	27003761
KARPAS299	Antiproliferative assay		72 hrs	Antiproliferative activity against human KARPAS299 cells incubated for 72 hrs by cell titer-glo assay, IC50 = 0.031 μM.	27003761
SUP-M2	Antiproliferative assay		72 hrs	Antiproliferative activity against human SUP-M2 cells expressing ALK protein incubated for 72 hrs by cell titer-glo assay, IC50 = 0.041 μM.	27003761
BAF3	Function assay		72 hrs	Inhibition of EML4-ALK L1196M mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.067 μM.	27003761
NCI-H2228	Antiproliferative assay		72 hrs	Antiproliferative activity against human NCI-H2228 cells expressing ALK protein incubated for 72 hrs by cell titer-glo assay, IC50 = 0.068 μM.	27003761
MV411	Antiproliferative assay		72 hrs	Antiproliferative activity against human MV411 cells incubated for 72 hrs by cell titer-glo assay, IC50 = 0.081 μM.	27003761
SR786	Antiproliferative assay		72 hrs	Antiproliferative activity against human SR786 cells expressing ALK protein incubated for 72 hrs by cell titer-glo assay, IC50 = 0.081 μM.	27003761
BAF3	Function assay		72 hrs	Inhibition of EML4-ALK G1202R mutant (unknown origin) expressed in mouse BAF3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay, IC50 = 0.897 μM.	27003761
BA/F3	Cytotoxicity assay		72 hrs	Cytotoxicity against mouse IL-3 dependent BA/F3 cells incubated for 72 hrs by cell titer-glo assay, IC50 = 2.104 μM.	27003761
KM12	Function assay		2 hrs	Inhibition of TPM3-TRKA phosphorylation in human KM12 cells at low concentration after 2 hrs by Western blot analysis	27003761
KM12	Function assay		2 hrs	Inhibition of TPM3-TRKA phosphorylation in human KM12 cells assessed as suppression of MAPK phosphorylation at low concentration after 2 hrs by Western blot analysis	27003761
KM12	Function assay		2 hrs	Inhibition of TPM3-TRKA phosphorylation in human KM12 cells assessed as suppression of PLCgamma1 phosphorylation at low concentration after 2 hrs by Western blot analysis	27003761
KM12	Function assay		2 hrs	Inhibition of TPM3-TRKA phosphorylation in human KM12 cells assessed as suppression of AKT phosphorylation at low concentration after 2 hrs by Western blot analysis	27003761
KM12	Function assay		2 hrs	Inhibition of TPM3-TRKA phosphorylation in human KM12 cells assessed as suppression of S6 phosphorylation at low concentration after 2 hrs by Western blot analysis	27003761
KARPAS299	Function assay		2 hrs	Inhibition of NPM/ALK autophosphorylation in human KARPAS299 cells at very low concentration after 2 hrs by Western blot analysis	27003761
NCI-H2228	Function assay		2 hrs	Inhibition of NPM/ALK autophosphorylation in human NCI-H2228 cells at very low concentration after 2 hrs by Western blot analysis	27003761
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

Entrectinib是一種口服生物可利用的泛-TrkA/B/C，ROS1 和 ALK 抑制劑，IC50范圍為 0.1~1.7 nM。Entrectinib (RXDX-101) 可誘導(dǎo)自噬。Phase 2。

靶點(diǎn)

TrkA ^[1]

TrkB ^[1]

TrkC ^[1]

ROS1 ^[1]

ALK ^[1]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗(yàn)信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT05770544	Recruiting	Solid Tumor\|Haematological Malignancy\|Malignancy\|Malignant Neoplasm\|Lymphoproliferative Disorders\|Neoplasms by Histologic Type\|Neoplasms by Site\|Cancer\|Brain Neoplasms\|Melanoma\|Glioma	Cancer Research UK\|University of Manchester\|University of Birmingham\|Royal Marsden NHS Foundation Trust\|Hoffmann-La Roche	June 2024	Phase 2\|Phase 3
NCT04551495	Recruiting	Invasive Lobular Breast Carcinoma\|ER+ Breast Cancer\|HER2-negative Breast Cancer	Jules Bordet Institute\|Hoffmann-La Roche	January 14 2021	Phase 2
NCT04226833	Completed	Hepatic Insufficiency	Hoffmann-La Roche	February 11 2020	Phase 1
NCT03796013	Completed	Healthy Volunteers	Genentech Inc.	January 10 2019	Phase 1

參考文獻(xiàn)
https://pubmed.ncbi.nlm.nih.gov/26457764/ http://mct.aacrjournals.org/content/8/12_Supplement/A244.short http://cancerres.aacrjournals.org/content/75/15_Supplement/5390 https://pubmed.ncbi.nlm.nih.gov/36101520/ https://pubmed.ncbi.nlm.nih.gov/33229458/ + 展開(kāi)

參考文獻(xiàn)

https://pubmed.ncbi.nlm.nih.gov/26457764/
http://mct.aacrjournals.org/content/8/12_Supplement/A244.short
http://cancerres.aacrjournals.org/content/75/15_Supplement/5390

https://pubmed.ncbi.nlm.nih.gov/36101520/
https://pubmed.ncbi.nlm.nih.gov/33229458/

+ 展開(kāi)

化學(xué)信息&溶解度

分子量	560.64	分子式	C₃₁H₃₄F₂N₆O₂
CAS號(hào)	1108743-60-7	SDF	Download Entrectinib SDF
Smiles	CN1CCN(CC1)C2=CC(=C(C=C2)C(=O)NC3=NNC4=C3C=C(C=C4)CC5=CC(=CC(=C5)F)F)NC6CCOCC6
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 100 mg/mL ( (178.36 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 100 mg/mL (178.36 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (178.36 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 25 mg/mL (44.59 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (178.36 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 75 mg/mL (133.77 mM)

Water : Insoluble

DMSO : 100 mg/mL ( (178.36 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Ethanol : 100 mg/mL (178.36 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解配方批次：現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑				動(dòng)物體內(nèi)配方計(jì)算器
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
澄清溶液	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O 該配方已經(jīng)過(guò)Selleck實(shí)驗(yàn)室實(shí)測(cè)。如果上述溶解方案不能滿(mǎn)足您的需求，可聯(lián)系Selleck銷(xiāo)售提供定制化測(cè)試。	5.000mg/ml (8.92mM)	以 1 mL 工作液為例，取50μL100mg/ml的澄清DMSO儲(chǔ)備液加到400μL PEG300中，混合均勻使其澄清；向上述體系中加入50μLTween80，混合均勻使其澄清；然后繼續(xù)加入500μL ddH2O定容至 1 mL。工作液請(qǐng)現(xiàn)配現(xiàn)用！
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。
均勻懸濁液	CMC-NA	≥5mg/ml	以 1 mL 工作液為例，取 5 mg該產(chǎn)品加到 1 ml CMC-NA 溶液中，混合均勻，即可得工作液濃度為 5 mg/ml的均勻懸濁液。

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

技術(shù)支持

在訂購(gòu)、運(yùn)輸、儲(chǔ)存和使用我們的產(chǎn)品的任何階段，您遇到的任何問(wèn)題，均可以通過(guò)撥打我們的熱線(xiàn)電話(huà)400-668-6834，或者技術(shù)支持郵箱[email protected]，直接聯(lián)系到我們。我們會(huì)在24小時(shí)內(nèi)盡快聯(lián)系您。

操作手冊(cè)

如果有其他問(wèn)題，請(qǐng)給我們留言。

* 必填項(xiàng)

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):

Entrectinib

產(chǎn)品質(zhì)控

Entrectinib相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實(shí)驗(yàn)計(jì)算

技術(shù)支持