| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
NSC305787 is an ezrin inhibitor that exhibits anti-tumor activity 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) exhibits inhibitory activity against K7M2 osteosarcoma (OS) cell invasion mediated by ezrin. Moreover, NSC305787 (10 μM) inhibits the growth of OS metastasis in lung organ cultures 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 suppresses lung metastasis and seems to be more beneficial than NSC668394 in the mouse model. dynamic qualities [2].
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| References |
| Molecular Formula |
C25H30CL2N2O
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|---|---|
| Molecular Weight |
445.4245
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| Exact Mass |
444.173
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| CAS # |
785718-37-8
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| Related CAS # |
(Rac)-NSC305787 hydrochloride;53868-26-1
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| PubChem CID |
470998
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
597.2±45.0 °C at 760 mmHg
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| Flash Point |
315.0±28.7 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.646
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| LogP |
5.73
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
603
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=C([H])C(=C([H])C2=C1N=C(C([H])=C2C([H])(C1([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N1[H])O[H])C12C([H])([H])C3([H])C([H])([H])C([H])(C([H])([H])C([H])(C3([H])[H])C1([H])[H])C2([H])[H])Cl
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| InChi Key |
YNGQUUFYBFKLNH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C25H30Cl2N2O/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
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| Chemical Name |
[2-(1-adamantyl)-6,8-dichloroquinolin-4-yl]-piperidin-2-ylmethanol
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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 |
| 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 : ~6 mg/mL (~13.47 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.6 mg/mL (1.35 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 6.0 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: ≥ 0.6 mg/mL (1.35 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 6.0 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: ≥ 0.6 mg/mL (1.35 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 | 2.2451 mL | 11.2254 mL | 22.4507 mL | |
| 5 mM | 0.4490 mL | 2.2451 mL | 4.4901 mL | |
| 10 mM | 0.2245 mL | 1.1225 mL | 2.2451 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.
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