Entrectinib (Synonyms: 恩曲替尼; NMS-E628; RXDX-101)

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Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

Entrectinib (NMS-E628) 是口服有效的，可透過(guò)血腦屏障的，且具有中樞神經(jīng)活性的 TrkA/B/C, ROS1 和 ALK 抑制劑，其 IC₅₀ 值分別為 1, 3, 5, 12 和 7 nM。Entrectinib 誘導(dǎo)癌細(xì)胞凋亡和周期停滯，具有抗腫瘤活性，還可減輕博來(lái)霉素誘導(dǎo)的小鼠肺纖維化。

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Entrectinib Chemical Structure

CAS No. : 1108743-60-7

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可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3. 試用裝只面向終端客戶。

規(guī)格	價(jià)格	是否有貨
10 mM * 1 mL in DMSO	￥1073	In-stock
1 mg	￥371	In-stock
5 mg	￥870	In-stock
10 mg	￥1200	In-stock
25 mg	￥2088	In-stock
50 mg	￥3000	In-stock
100 mg	￥4500	In-stock
200 mg		詢價(jià)
500 mg		詢價(jià)

or 大包裝詢價(jià)

* Please select Quantity before adding items.

Customer Review

Other Forms of Entrectinib:

Entrectinib-d₈ In-stock
Entrectinib-d₄ 詢價(jià)
Entrectinib (Standard) 詢價(jià)

MCE 顧客使用本產(chǎn)品發(fā)表的 22 篇科研文獻(xiàn)

•Nat Biotechnol. 2024 Jul 24. [Abstract]
•Nature. 2021 Jun;594(7862):277-282. [Abstract]
•Science. 2017 Dec 1;358(6367):eaan4368. [Abstract]
•Adv Sci (Weinh). 2024 Dec 5:e2410360.
•Cell Rep Med. 2023 Jan 10;100911. [Abstract]
•Nat Commun. 2021 Feb 24;12(1):1261. [Abstract]

•Sci Data. 2024 Sep 19.
•Mol Syst Biol. 2023 Dec 18.
•Cell Rep. 2020 Aug 4;32(5):107994. [Abstract]
•J Mol Liq. 2024 Sep 1.
•iScience. 2023 May 29, 107006.
•Drug Des Dev Ther. 2020 Oct 23;14:4439-4449. [Abstract]
•Eur J Med Chem. 2020 Aug 30;207:112744. [Abstract]
•Clin Chim Acta. 2018 Oct;485:298-304. [Abstract]
•Oncol Rep. 2018 Aug;40(2):635-646. [Abstract]
•Mol Cancer Ther. 2017 Oct;16(10):2130-2143. [Abstract]
•Separations. 2023 Sep 11, 10(9), 494.
•J Neuropathol Exp Neurol. 2021 Mar 22;80(4):345-353. [Abstract]
•Fundam Clin Pharmacol. 2021 Feb 1. [Abstract]
•Eur J Drug Metab Pharmacokinet. 2021 Jul 18;1-11. [Abstract]
•University of California. 2024.
•bioRxiv. 04 Nov 2021.

: Entrectinib purchased from MCE. Usage Cited in: Cell Rep. 2020 Aug 4;32(5):107994. [Abstract]; Immunoblot analysis of protein expression or modification in lysates of IMPETPR-NTRK1 cells treated with 10 nM Entrectinib for 0-24 h. pTRKA remained completely inhibited at 18 and 24 h, indicating that Entrectinib is still effectively inhibiting its direct target.

: Entrectinib purchased from MCE. Usage Cited in: Mol Cancer Ther. 2017 Oct;16(10):2130-2143. [Abstract]; KM12 or CR20 cells are treated with increasing concentrations of Cabozantinib, Entrectinib or LOXO-101 for 3 hours. Cell lysates are immunoblotted to detect the indicated proteins.

Entrectinib 相關(guān)產(chǎn)品

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TrkA TrkB TrkC Trk

生物活性
純度 & 產(chǎn)品資料
參考文獻(xiàn)

生物活性

Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC₅₀ values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice^[1]^[2]^[3].

IC₅₀ & Target

IC50: 1 nM (TrkA), 3 nM (TrkB), 5 nM (TrkC), 12 nM (ROS1), 7 nM (ALK)^[2].

細(xì)胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
A549	IC₅₀	7.46 μM Compound: Entrectinib	Antiproliferative activity against EGFR-positive human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against EGFR-positive human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 34534734]
BaF3	IC₅₀	0.003 μM Compound: 2; entrectinib	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 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	[PMID: 27003761]
BaF3	IC₅₀	0.003 μM Compound: 2; entrectinib	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 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	[PMID: 27003761]
BaF3	IC₅₀	0.003 μM Compound: 2; entrectinib	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 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	[PMID: 27003761]
BaF3	IC₅₀	0.005 μM Compound: 2; entrectinib	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 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	[PMID: 27003761]
BaF3	IC₅₀	0.028 μM Compound: 2; entrectinib	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 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	[PMID: 27003761]
BaF3	IC₅₀	0.067 μM Compound: 2; entrectinib	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 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	[PMID: 27003761]
BaF3	IC₅₀	0.897 μM Compound: 2; entrectinib	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 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	[PMID: 27003761]
BaF3	IC₅₀	2.104 μM Compound: 2; entrectinib	Cytotoxicity against mouse IL-3 dependent BA/F3 cells incubated for 72 hrs by cell titer-glo assay Cytotoxicity against mouse IL-3 dependent BA/F3 cells incubated for 72 hrs by cell titer-glo assay	[PMID: 27003761]
KARPAS-299	IC₅₀	0.031 μM Compound: 2; entrectinib	Antiproliferative activity against human KARPAS299 cells incubated for 72 hrs by cell titer-glo assay Antiproliferative activity against human KARPAS299 cells incubated for 72 hrs by cell titer-glo assay	[PMID: 27003761]
KARPAS-299	IC₅₀	0.076 μM Compound: Entrectinib	Antiproliferative activity against NPM-ALK addicted human KARPAS-299 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against NPM-ALK addicted human KARPAS-299 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 34534734]
KARPAS-299	IC₅₀	31 nM Compound: 84	Antiproliferative activity against human KARPAS299 cells incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human KARPAS299 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 31077998]
KM12	IC₅₀	0.0017 μM Compound: 4-3; RXDX-101	Antiproliferative activity against human KM12 cells after 72 hrs Antiproliferative activity against human KM12 cells after 72 hrs	[PMID: 30188734]
KM12	IC₅₀	0.012 μM Compound: Entrectinib	Cytotoxicity against human KM12 cells assessed as reduction in cell viability incubated for 72 hrs by resazurin based assay Cytotoxicity against human KM12 cells assessed as reduction in cell viability incubated for 72 hrs by resazurin based assay	[PMID: 33652352]
KM12	IC₅₀	0.017 μM Compound: 2; entrectinib	Antiproliferative activity against human KM12 cells expressing TRKA protein incubated for 72 hrs by cell titer-glo assay Antiproliferative activity against human KM12 cells expressing TRKA protein incubated for 72 hrs by cell titer-glo assay	[PMID: 27003761]
KM12	IC₅₀	0.057 μM Compound: Entrectinib	Antiproliferative activity against TPM3-NTRK1-addicted human KM12 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against TPM3-NTRK1-addicted human KM12 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 34534734]
KM12	IC₅₀	17 nM Compound: 84	Antiproliferative activity against human KM12 cells incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human KM12 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 31077998]
KM12	IC₅₀	4.3 nM Compound: Entrectinib	Antiproliferative activity against human KM12 cells expressing TPM3-TRKA assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay Antiproliferative activity against human KM12 cells expressing TPM3-TRKA assessed as reduction in cell viability measured after 3 days by Celltiter-Glo assay	[PMID: 32550985]
MV4-11	IC₅₀	0.081 μM Compound: 2; entrectinib	Antiproliferative activity against human MV411 cells incubated for 72 hrs by cell titer-glo assay Antiproliferative activity against human MV411 cells incubated for 72 hrs by cell titer-glo assay	[PMID: 27003761]
MV4-11	IC₅₀	81 nM Compound: 84	Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human MV4-11 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 31077998]
NCI-H2228	IC₅₀	0.068 μM Compound: 2; entrectinib	Antiproliferative activity against human NCI-H2228 cells expressing ALK protein incubated for 72 hrs by cell titer-glo assay Antiproliferative activity against human NCI-H2228 cells expressing ALK protein incubated for 72 hrs by cell titer-glo assay	[PMID: 27003761]
NCI-H2228	IC₅₀	0.254 μM Compound: Entrectinib	Antiproliferative activity against EML4-ALK addicted human H2228 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against EML4-ALK addicted human H2228 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 34534734]
NCI-H2228	IC₅₀	68 nM Compound: 84	Antiproliferative activity against human NCI-H2228 cells incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human NCI-H2228 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 31077998]
SH-SY5Y	IC₅₀	1.6 μM Compound: Entrectinib	Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay Anticancer activity against human SH-SY5Y cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay	[PMID: 36208544]
SK-N-AS	IC₅₀	4.47 μM Compound: Entrectinib	Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay Anticancer activity against human SK-N-AS cells assessed as reduction in cell viability incubated for 48 hrs by resazurin dye based fluorescence assay	[PMID: 36208544]
SU-DHL-1	IC₅₀	0.024 μM Compound: 2; entrectinib	Antiproliferative activity against human SU-DHL1 cells expressing ALK protein incubated for 72 hrs by cell titer-glo assay Antiproliferative activity against human SU-DHL1 cells expressing ALK protein incubated for 72 hrs by cell titer-glo assay	[PMID: 27003761]
SU-DHL-1	IC₅₀	20 nM Compound: 84	Antiproliferative activity against human SU-DHL1 cells incubated for 48 hrs by sulforhodamine B assay Antiproliferative activity against human SU-DHL1 cells incubated for 48 hrs by sulforhodamine B assay	[PMID: 31077998]

體外研究
(In Vitro)

Entrectinib (100, 200, 400 nM; 24 h) 緩解 TGF-β1 誘導(dǎo)的小鼠肺成纖維細(xì)胞的激活^[1]。
Entrectinib(100, 200, 400 nM; 24 h) 抑制 TGF-β1 誘導(dǎo)的小鼠肺上皮細(xì)胞上皮間質(zhì)轉(zhuǎn)化^[1]。
Entrectinib (10, 50, 250 nM; 2 h) 消除 KM12 細(xì)胞中 TPM3-TRKA 的自身磷酸化，同時(shí)完全抑制 PLCg1、AKT 和 MAPK 的磷酸化^[2]。
Entrectinib (10, 50, 250 nM; 24, 48 h) 誘導(dǎo) KM12 細(xì)胞周期停滯 (24 小時(shí)) 和凋亡 (48 小時(shí))^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:	Mouse lung fibroblasts cells
Concentration:	100, 200, 400 nM
Incubation Time:	24 h
Result:	Reduced the protein expression levels of α-SMA, collagen I and fibronectin in the TGF-β1-treated fibroblasts.

Western Blot Analysis^[1]

Cell Line:	Mouse lung epithelial cells
Concentration:	100, 200, 400 nM
Incubation Time:	24 h
Result:	Significantly increased the expression of the epithelial marker Ecadherin and decreased the expression of the mesenchymal markers N-cadherin and Vimentin.

Apoptosis Analysis^[2]

Cell Line:	KM12 cells
Concentration:	10, 50, 250 nM
Incubation Time:	24, 48 h
Result:	Induced accumulation of cells in the G1 phase of the cell cycle at 24 hours treatment, followed by apoptosis induction at 48 hours.

體內(nèi)研究
(In Vivo)

Entrectinib (20, 40, 60 mg/kg; i.g.; single daily for 7 days) 減輕 Bleomycin 誘導(dǎo)的小鼠肺纖維化^[1]。
Entrectinib (30, 60 mg/kg; p.o.; twice daily for 10 consecutive days) 可誘導(dǎo)荷瘤小鼠中異種移植腫瘤的消退，包括 TRKA 依賴性結(jié)直腸癌 KM12、ROS1 驅(qū)動(dòng)的腫瘤和幾種不同組織來(lái)源的 ALK 依賴性模型，包括腦局部肺模型癌轉(zhuǎn)移^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57BL/6 mice (6-8 weeks old, 20-25 g; Bleomycin-induced pulmonary fibrosis model)^[1].
Dosage:	20, 40, 60 mg/kg
Administration:	Intragastric Administration; single daily for 7 days.
Result:	Significantly improved lung function in the pulmonary fibrosis model mice.

Clinical Trial

分子量

560.64

Formula

C₃₁H₃₄F₂N₆O₂

CAS 號(hào)

1108743-60-7

性狀

固體

顏色

Off-white to light yellow

中文名稱

恩曲替尼

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : ≥ 31 mg/mL (55.29 mM; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	1.7837 mL	8.9184 mL	17.8368 mL
5 mM	0.3567 mL	1.7837 mL	3.5674 mL
10 mM	0.1784 mL	0.8918 mL	1.7837 mL

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.5 mg/mL (4.46 mM); 澄清溶液
方案二

請(qǐng)依序添加每種溶劑： 5% DMSO 95% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.46 mM); 澄清溶液
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.71 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案四

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.71 mM); 懸濁液; 超聲助溶

此方案可獲得 2.08 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案五

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (3.71 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

以下溶解方案，請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配，在短期內(nèi)盡快用完。以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的方式助溶。

方案一

請(qǐng)依序添加每種溶劑： 0.5% Methyl cellulose/0.5% Tween-80 in Saline water
Solubility: 5 mg/mL (8.92 mM); 懸濁液; 超聲助溶

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過(guò) 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購(gòu)。，Tween 80，均可在 MCE 網(wǎng)站選購(gòu)。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過(guò)該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國(guó)技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過(guò)半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.79%

選擇批次：

Data Sheet (650 KB) SDS (393 KB)

COA (290 KB) HNMR (281 KB) LCMS (94 KB) 元素分析報(bào)告 (213 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Miao Y, et al. Entrectinib ameliorates bleomycin-induced pulmonary fibrosis in mice by inhibiting TGF-β1 signaling pathway. Int Immunopharmacol. 2022 Dec;113(Pt B):109427. [Content Brief]

[2]. Ardini E, et al. Entrectinib, a Pan-TRK, ROS1, and ALK Inhibitor with Activity in Multiple Molecularly Defined Cancer Indications. Mol Cancer Ther. 2016 Apr;15(4):628-39. [Content Brief]

[3]. Iyer R, et al. Entrectinib is a potent inhibitor of Trk-driven neuroblastomas in a xenograft mouse model. Cancer Lett. 2016 Mar 28;372(2):179-86. [Content Brief]

Entrectinib 相關(guān)分類

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.7837 mL	8.9184 mL	17.8368 mL	44.5919 mL
	5 mM	0.3567 mL	1.7837 mL	3.5674 mL	8.9184 mL
	10 mM	0.1784 mL	0.8918 mL	1.7837 mL	4.4592 mL
	15 mM	0.1189 mL	0.5946 mL	1.1891 mL	2.9728 mL
	20 mM	0.0892 mL	0.4459 mL	0.8918 mL	2.2296 mL
	25 mM	0.0713 mL	0.3567 mL	0.7135 mL	1.7837 mL
	30 mM	0.0595 mL	0.2973 mL	0.5946 mL	1.4864 mL
	40 mM	0.0446 mL	0.2230 mL	0.4459 mL	1.1148 mL
	50 mM	0.0357 mL	0.1784 mL	0.3567 mL	0.8918 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Entrectinib (Synonyms: 恩曲替尼; NMS-E628; RXDX-101)

Customer Review

Other Forms of Entrectinib:

MCE 顧客使用本產(chǎn)品發(fā)表的 22 篇科研文獻(xiàn)

Entrectinib 相關(guān)產(chǎn)品

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•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 Trk Receptor 亞型特異性產(chǎn)品:

生物活性

純度 & 產(chǎn)品資料

參考文獻(xiàn)

摩爾計(jì)算器

稀釋計(jì)算器

Entrectinib 相關(guān)分類

完整儲(chǔ)備液配制表

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Entrectinib (Synonyms: 恩曲替尼; NMS-E628; RXDX-101)

Customer Review

Other Forms of Entrectinib:

Entrectinib 相關(guān)抗體

MCE 顧客使用本產(chǎn)品發(fā)表的 22 篇科研文獻(xiàn)

Entrectinib 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

查看 Trk Receptor 亞型特異性產(chǎn)品:

生物活性

純度 & 產(chǎn)品資料

參考文獻(xiàn)

Entrectinib 相關(guān)抗體:

摩爾計(jì)算器

稀釋計(jì)算器

Entrectinib 相關(guān)分類

完整儲(chǔ)備液配制表

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