Cat. No.: HY-12678

Entrectinib

(Synonyms: NMS-E628; RXDX-101)

30 Cited Publications

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Based on 30 publication(s) in Google Scholar

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.

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Pureté: 98.98%
CAS No.: 1108743-60-7
Formule: C₃₁H₃₄F₂N₆O₂
Masse moléculaire:560.64

Stockage:

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

Entrectinib Chemical Structure

CAS No.: 1108743-60-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (30)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

IC₅₀ & Target

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

Voir tous les produits spécifiques à Isoform Trk Receptor :

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]
A549	IC₅₀	7.46 μM Compound: Entrectinib	Antiproliferative activity against human A549 cells assessed as reduction in cell viability for 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability for 72 hrs by MTT assay	[PMID: 36095945]
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	0.078 μM Compound: Entrectinib	Antiproliferative activity against human KM12 cells assessed as reduction in cell viability for 72 hrs by MTT assay Antiproliferative activity against human KM12 cells assessed as reduction in cell viability for 72 hrs by MTT assay	[PMID: 36095945]
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]

In Vitro

Entrectinib (100, 200, 400 nM; 24 h) alleviates TGF-β1-induced activation of mouse lung fibroblasts^[1].
Entrectinib(100, 200, 400 nM; 24 h) inhibits TGF-β1-induced epithelial to mesenchymal transition of mouse lung epithelial cells^[1].
Entrectinib (10, 50, 250 nM; 2 h) abolishes autophosphorylation of TPM3-TRKA, concomitant with complete inhibition of the phosphorylation of PLCg1, AKT, and MAPK in KM12 cells^[2].
Entrectinib (10, 50, 250 nM; 24, 48 h) induce KM12 cells cycle arrest (24 h) and apoptosis (48 h)^[2].

MedChemExpress (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.

In Vivo

Entrectinib (20, 40, 60 mg/kg; i.g.; single daily for 7 days) attenuates bleomycin-induced pulmonary fibrosis in mice^[1].
Entrectinib (30, 60 mg/kg; p.o.; twice daily for 10 consecutive days) induces regression of xenograft tumors in tumor-bearing mice, including TRKA-dependent colorectal cancer KM12, ROS1-driven tumors, and several ALK-dependent models of different tissue origins, including brain-localized lung model cancer metastasis^[2].

MedChemExpress (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.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1108743-60-7
Appearance Solid
Masse moléculaire 560.64
Formule C₃₁H₃₄F₂N₆O₂
Color Off-white to light yellow
SMILES

O=C(NC1=NNC2=C1C=C(CC3=CC(F)=CC(F)=C3)C=C2)C4=C(NC5CCOCC5)C=C(N6CCN(C)CC6)C=C4
Synonyms

NMS-E628; RXDX-101
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (30)

All WBApoptosis Analysis

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Journal Impact Factor

Nature

NF1 mutation drives neuronal activity-dependent initiation of optic glioma. [Abstract]

2021 Jun;594(7862):277-282. PMID: 34040258
Science

The target landscape of clinical kinase drugs. [Abstract]

2017 Dec 1;358(6367):eaan4368. PMID: 29191878
Nat Biotechnol

Large-scale discovery of chromatin dysregulation induced by oncofusions and other protein-coding variants. [Abstract]

2025 Jun;43(6):996-1010. PMID: 39048711
Nat Commun

Gilteritinib overcomes lorlatinib resistance in ALK-rearranged cancer. [Abstract]

2021 Feb 24;12(1):1261. PMID: 33627640

Entrectinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Feb 24;12(1):1261. [Abstract]

Phospho-ALK and its downstream signals in MR347 cells were evaluated by western blotting after the treatment of the indicated concentration of inhibitors (Entrectinib, 100 nM) for 6h.

Entrectinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Feb 24;12(1):1261. [Abstract]

Phospho-ALK in each EML4- ALK mutations expressing Ba/F3 cells were evaluated by western blotting. Cells were treated with the indicated concentrations of entrectinib (0, 50, 100 nM) for 3 h.

Entrectinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Feb 24;12(1):1261. [Abstract]

Suppression of phospho-NTRK1 and its downstream signals in KM12 cells were evaluated by western blotting. Cells were treated with the entrectinib (30 nM) or gilteritinib for 6 h

Entrectinib purchased from MedChemExpress. Usage Cited in: Nat Commun. 2021 Feb 24;12(1):1261. [Abstract]

Apoptosis assay by flow cytometry analysis with Annexin-V and PI staining after 72 h of 100 nM entrectinib or gilteritinib treatment to KM12 cells. The percentage of cells undergoing apoptosis is shown in red.
Adv Sci (Weinh)

Targeted SPP1 Inhibition of Tumor-Associated Myeloid Cells Effectively Decreases Tumor Sizes. [Abstract]

2024 Dec 5:e2410360. PMID: 39639496
Cell Rep Med

Using patient-derived organoids to predict locally advanced or metastatic lung cancer tumor response: A real-world study. [Abstract]

2023 Feb 21;4(2):100911. PMID: 36657446
Mol Syst Biol

Illuminating phenotypic drug responses of sarcoma cells to kinase inhibitors by phosphoproteomics. [Abstract]

2024 Jan;20(1):28-55. PMID: 38177929
Sci Data

High-throughput drug screening identifies novel therapeutics for Low Grade Serous Ovarian Carcinoma. [Abstract]

2024 Sep 19;11(1):1024. PMID: 39300112
Cell Rep

Inhibition of MEK1/2 Forestalls the Onset of Acquired Resistance to Entrectinib in Multiple Models of NTRK1-Driven Cancer. [Abstract]

2020 Aug 4;32(5):107994. PMID: 32755586

Entrectinib purchased from MedChemExpress. 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.
Eur J Med Chem

Discovery of (E)-N-(4-methyl-5-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thiazol-2-yl)-2-(4-methylpiperazin-1-yl)acetamide (IHMT-TRK-284) as a novel orally available type II TRK kinase inhibitor capable of overcoming multiple resistant mutants. [Abstract]

2020 Aug 30;207:112744. PMID: 32949955
Mol Cancer Ther

Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers. [Abstract]

2017 Oct;16(10):2130-2143. PMID: 28751539

Entrectinib purchased from MedChemExpress. 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.
J Mol Liq

2024 Sep 1.
Drug Des Devel Ther

LC-MS/MS Estimation of the Anti-Cancer Agent Tandutinib Levels in Human Liver Microsomes: Metabolic Stability Evaluation Assay. [Abstract]

2020 Oct 23;14:4439-4449. PMID: 33122888
Eur J Pharm Sci

Repurposing of FDA-approved drugs by targeting SIRT2 to alleviate inflammatory response and kidney injury. [Abstract]

2025 Sep 27:214:107296. PMID: 41022315
iScience

Overcoming MET-mediated resistance in oncogene-driven NSCLC. [Abstract]

2023 May 29;26(7):107006. PMID: 37534190
Oncol Rep

Evaluation of anticancer agents using patient-derived tumor organoids characteristically similar to source tissues. [Abstract]

2018 Aug;40(2):635-646. PMID: 29917168
Bioengineering (Basel)

Precision Oncology for High-Grade Gliomas: A Tumor Organoid Model for Adjuvant Treatment Selection. [Abstract]

2025 Oct 19;12(10):1121. PMID: 41155119
Diagnostics (Basel)

Application of Drug Testing Platforms in Circulating Tumor Cells and Validation of a Patient-Derived Xenograft Mouse Model in Patient with Primary Intracranial Ependymomas with Extraneural Metastases. [Abstract]

2023 Mar 24;13(7):1232. PMID: 37046450
J Neuropathol Exp Neurol

NTRK Fusions Can Co-Occur With H3K27M Mutations and May Define Druggable Subclones Within Diffuse Midline Gliomas. [Abstract]

2021 Mar 22;80(4):345-353. PMID: 33749791
Clin Chim Acta

Investigation of metabolic degradation of new ALK inhibitor: Entrectinib by LC-MS/MS. [Abstract]

2018 Oct:485:298-304. PMID: 30006284
Separations

2023 Sep 11, 10(9), 494.
Fundam Clin Pharmacol

Inhibition of organic cation transporter 3 activity by tyrosine kinase inhibitors. [Abstract]

2021 Oct;35(5):919-929. PMID: 33523504
Eur J Drug Metab Pharmacokinet

Differential Inhibition of Equilibrative Nucleoside Transporter 1 (ENT1) Activity by Tyrosine Kinase Inhibitors. [Abstract]

2021 Sep;46(5):625-635. PMID: 34275128
chemRxiv

2026 Apr 6.
Albert Einstein College of Medicine

2025.
ChemRxiv

2025 Jun 11.
bioRxiv

Loss of CARM1 alters the developmental programming of Glioma stem-like cells and creates a druggable NGFR/NTRK dependency. [Abstract]

2025 Apr 17:2025.04.11.647869. PMID: 40321217
Res Sq

2025 Apr 14.
University of California

2024.
bioRxiv

04 Nov 2021.

Solvant et solubilité

In Vitro:

DMSO : ≥ 31 mg/mL (55.29 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 2.5 mg/mL (4.46 mM); Clear solution

Protocol 2

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.46 mM); Clear solution

Protocol 3

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 4

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.08 mg/mL (3.71 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 5

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (3.71 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 0.5% Methyl cellulose/0.5% Tween-80 in Saline water

Solubility: 5 mg/mL (8.92 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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+
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Références

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	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

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Entrectinib

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Entrectinib

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