(Rac)-NSC305787 hydrochloride
Based on 10 publication(s) in Google Scholar
NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, has antitumor activity.
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- Pureté: 98.18%
- CAS No.: 53868-26-1
- Formule: C25H31Cl3N2O
- Masse moléculaire:481.89
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Stockage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) (Rac)-NSC305787 hydrochloride
More- Cell. 2026 Apr 2;189(7):1942-1956.e26. [Abstract]
- Cell. 2023 Jan 5;186(1):112-130.e20. [Abstract]
- Adv Sci (Weinh). 2026 Mar;13(16):e13310. [Abstract]
- Sci Adv. 2025 Oct 24;11(43):eads9181. [Abstract]
- Life Sci. 2020 Aug 1:254:117681. [Abstract]
- Front Cell Dev Biol. 2021 Sep 3;9:663207. [Abstract]
- PLoS Pathog. 2019 May 9;15(5):e1007737. [Abstract]
- J Cell Mol Med. 2022 Apr;26(7):2089-2103. [Abstract]
- Am J Physiol Renal Physiol. 2025 Aug 1;329(2):F269-F283. [Abstract]
- Biochem Biophys Res Commun. 2024 Apr 9:703:149685. [Abstract]
Customer Validation & Images
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WB
Activité biologique
NSC305787 hydrochloride is an inhibitor of ezrin with a Kd of 5.85 μM, and has antitumor activity. NSC305787 inhibits PKCΙ phosphorylation of Ezrin, Moesin, Radixin, MBP, with IC50s of 8.3, 9.4, 55, 58.9 μM, respectively. NSC305787 binds to PKCΙ with a Kd value of 172.4 μM, and inhibits ezrin T567 phosphorylation primarily via its binding to ezrin and not through inhibition of PKCΙ kinase activity. NSC305787 (1, 10 μM) shows inhibitory activity against ezrin-mediated invasion of K7M2 osteosarcoma (OS) cells. Moreover, NSC305787 (10 μM) reduces cell motility phenotypes in zebrafish and blocks OS metastatic growth in lung organ culture[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 53868-26-1
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Appearance Solid
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Masse moléculaire 481.89
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Formule C25H31Cl3N2O
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Color White to off-white
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SMILES
OC(C1CCCCN1)C2=CC(C3(C[C@H](C4)C5)C[C@H]5C[C@H]4C3)=NC(C(Cl)=C6)=C2C=C6Cl.[H]Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (10)
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Journal Impact Factor
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Most Recent
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Cell
Ferritin aggregation cell engager for CAR T avidity engineering against refractory leukemias. [Abstract]2026 Apr 2;189(7):1942-1956.e26. PMID: 41806835 -
Cell
SARS-CoV-2 replication in airway epithelia requires motile cilia and microvillar reprogramming. [Abstract]2023 Jan 5;186(1):112-130.e20. PMID: 36580912 -
Adv Sci (Weinh)
2026 Mar;13(16):e13310. PMID: 41589654 -
Sci Adv
The chloride intracellular channel 1 (CLIC1) is essential for microglial morphodynamics and neuroinflammation. [Abstract]2025 Oct 24;11(43):eads9181. PMID: 41124273 -
Life Sci
Ezrin T567 phosphorylation regulates migration and invasion of ectopic endometrial stromal cells by changing actin cytoskeleton. [Abstract]2020 Aug 1:254:117681. PMID: 32380081
(Rac)-NSC305787 hydrochloride purchased from MedChemExpress. Usage Cited in: Life Sci. 2020 Aug 1:254:117681. [Abstract]
NSC305787 considerably inhibits the expression of p-ezrin, RhoA, RohC and ROCK1 without altering cellular ezrin levels at 2.5 μM and 5 μM.
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Front Cell Dev Biol
2021 Sep 3;9:663207. PMID: 34540823 -
PLoS Pathog
A streptococcal Fic domain-containing protein disrupts blood-brain barrier integrity by activating moesin in endothelial cells. [Abstract]2019 May 9;15(5):e1007737. PMID: 31071198 -
J Cell Mol Med
CD44/ERM/F-actin complex mediates targeted nuclear degranulation and excessive neutrophil extracellular trap formation during sepsis. [Abstract]2022 Apr;26(7):2089-2103. PMID: 35146909 -
Am J Physiol Renal Physiol
Renal ischemia-reperfusion injury triggers proximal tubular apoptosis and NHE3 dysfunction via p38MAPK/ezrin signaling pathway. [Abstract]2025 Aug 1;329(2):F269-F283. PMID: 40610014 -
Biochem Biophys Res Commun
Inhibition of ezrin phosphorylation by NSC305787 attenuates procaterol-stimulated ciliary beating in airway cilia. [Abstract]2024 Apr 9:703:149685. PMID: 38373381
Solvant et solubilité
DMSO : 8 mg/mL (16.60 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : < 0.1 mg/mL (insoluble)
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 1.25 mg/mL (2.59 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 1.25 mg/mL (2.59 mM); Clear solution
This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
Human umbilical vein endothelial cells (HUVECs; 2.5 × 104/well) are seeded in a 96-well plate in endothelial growth media-2. Following formation of a confluent HUVEC monolayer (∼32 h), endothelial growth media-2 is aspirated and a layer of osteosarcoma (OS) cells (1.0 × 104 cells/well) is added to Dulbecco’s modified Eagle medium containing NSC305787. This specific time point is accepted as 0 h of treatment, and invasion is monitored during the subsequent 5 h by measuring changes in resistance at the cell-electrode interphase. The cell index is calculated according to the following formula: cell index = (Rt – R0)/F, where Rt is resistance at time point t, R0 is background resistance (measured with media alone, no cells) and F is frequency at which the measurement is taken (10 kHz)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[2]
The Osx-Cre+p53fl/flpRBfl/fl transgenic mouse model of osteosarcoma is used in the assay. Mice are treated with 240 μg/kg/day NSC305787, 226 μg/kg/day NSC668394, or vehicle (DMSO, 1%) once daily, five times a week by i.p. injection in a volume of 100 μL. At the end of the study, lung and tumor samples are isolated upon necropsy. Half of each sample is flash frozen immediately in liquid nitrogen, and the other half is fixed in 10% formalin for 18-24 h, transferred to 70% ethanol, and stored at room temperature[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Bulut G, et al. Small molecule inhibitors of ezrin inhibit the invasive phenotype of osteosarcoma cells. Oncogene. 2012 Jan 19;31(3):269-81. [Content Brief]
[2]. Çelik H, et al. Ezrin Inhibition Up-regulates Stress Response Gene Expression. J Biol Chem. 2016 Jun 17;291(25):13257-70. [Content Brief]
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0752 mL | 10.3758 mL | 20.7516 mL | 51.8791 mL |
| 5 mM | 0.4150 mL | 2.0752 mL | 4.1503 mL | 10.3758 mL | |
| 10 mM | 0.2075 mL | 1.0376 mL | 2.0752 mL | 5.1879 mL | |
| 15 mM | 0.1383 mL | 0.6917 mL | 1.3834 mL | 3.4586 mL |
(Rac)-NSC305787 hydrochloride Related Classifications
HY-18931A Related Classifications
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