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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Entrectinib Chemical Structure
CAS No. : 1108743-60-7
This product is a controlled substance and not for sale in your territory.
Based on 20 publication(s) in Google Scholar
Other Forms of Entrectinib:
Entrectinib-d4
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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.
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.
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Description
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].
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.
Entrectinib Related Antibodies
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.
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
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.
Preparing Stock Solutions
ConcentrationSolventMass
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
View the Complete Stock Solution Preparation Table
*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.
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
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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 μLDMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 5
Add each solvent one by one: 10% DMSO 90% Corn Oil
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 μLDMSO stock solution (20.8 mg/mL) to 900 μLCorn oil, and mix evenly.
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:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[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]
[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.
[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.
[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.
Complete Stock Solution Preparation Table
*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.
Optional Solvent
ConcentrationSolventMass
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
Entrectinib Related Classifications
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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