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Purity: ≥98%
NSC305787 HCl, the hydrochloride salt of NSC305787, is a novel, potent and selective small molecule inhibitor of ezrin with a Kd of 5.85 μM, it inhibits the phosphorylation of ezrin caused by PKCΙ with an IC50 of 8.3 μM, and has antitumor activity. Ezrin is a key driver of tumor progression and metastatic spread of osteosarcoma. NSC-305787 HCl directly binds to ezrin and inhibits its functions in promoting invasive phenotype. NSC-305787 HCl reduces the incidence of lung metastasis in a genetically engineered mouse model of osteosarcoma.
| ln Vitro |
The ezrin inhibitor NSC305787 hydrochloride has anti-tumor action and a Kd of 5.85 μM. Ezrin, Moesin, Radixin, and MBP's PKCI phosphorylation is inhibited by NSC305787, with IC50 values of 8.3, 9.4, 55, and 58.9 μM, respectively. With a Kd value of 172.4 μM, NSC305787 binds to PKCI and primarily blocks ezrin T567 phosphorylation by binding to ezrin instead of PKCI kinase activity. NSC305787 (1, 10 μM) has inhibitory effect against K7M2 osteosarcoma (OS) cell invasion mediated by ezrin. Moreover, NSC305787 (10 μM) inhibits the growth of OS metastases in lung organ preparations and decreases the cell motility phenotype of zebrafish [1].
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| ln Vivo |
In mouse lungs, NSC305787 (0.240 mg/kg/day, intraperitoneal injection) prevents ezrin-dependent osteosarcoma from spreading [1]. In a transgenic mouse model of osteosarcoma (Osx-Cre+p53fl/flpRBfl/fl), NSC305787 (240 μg/kg, i.p.) significantly inhibits lung metastasis and seems to be more beneficial than NSC668394 in the mouse model. dynamic qualities [2].
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| References |
| Molecular Formula |
C25H31CL3N2O
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|---|---|
| Molecular Weight |
481.8854
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| Exact Mass |
480.15
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| CAS # |
53868-26-1
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| Related CAS # |
(Rac)-NSC305787;785718-37-8
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| PubChem CID |
54607543
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
31
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| Complexity |
603
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
JQALIVSYOXLOBE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H30Cl2N2O.ClH/c26-17-8-18-19(24(30)21-3-1-2-4-28-21)10-22(29-23(18)20(27)9-17)25-11-14-5-15(12-25)7-16(6-14)13-25;/h8-10,14-16,21,24,28,30H,1-7,11-13H2;1H
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| Chemical Name |
(2-(adamantan-1-yl)-6,8-dichloroquinolin-4-yl)(piperidin-2-yl)methanol hydrochloride
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| Synonyms |
NSC-305787HCl; NSC 305787 Hydrochloride; NSC305787 Hydrochloride; NSC-305787 HCl; NSC 305787 HCl; NSC305787 HCl;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~8 mg/mL (~16.60 mM)
H2O : < 0.1 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (2.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (2.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0752 mL | 10.3758 mL | 20.7516 mL | |
| 5 mM | 0.4150 mL | 2.0752 mL | 4.1503 mL | |
| 10 mM | 0.2075 mL | 1.0376 mL | 2.0752 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
 The small molecule inhibitors of ezrin up-regulate the integrated stress response-related genes.J Biol Chem.2016 Jun 17;291(25):13257-70. |
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 Pharmacological inhibition of ezrin by NSC305787 and NSC668394 up-regulates the expression of integrated stress response signature genes in a dose-dependent manner.J Biol Chem.2016 Jun 17;291(25):13257-70. |
 Suppression of ezrin expression leads to increased mRNA levels of downstream integrated stress response signaling effector genes and results in loss of transcriptional response to anti-ezrin compound.J Biol Chem.2016 Jun 17;291(25):13257-70. |
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