[CAS NO. 785718-37-8] (Rac)-NSC305787

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PRODUCTS SPECIFICATIONS [785718-37-8]

Catalog

HY-18931

Brand

MCE

CAS

785718-37-8

DESCRIPTION [785718-37-8]

Overview

MDL	-
Molecular Weight	445.42
Molecular Formula	C25H30Cl2N2O
SMILES	OC(C1CCCCN1)C2=CC(C3(C[C@H](C4)C5)C[C@H]5C[C@H]4C3)=NC(C(Cl)=C6)=C2C=C6Cl

For research use only. We do not sell to patients.

4 Publications Citing Use of MCE

Summary

NSC305787 is an inhibitor of ezrin with a K _d of 5.85 μM, inhibits the phosphorylation of ezrin caused by PKCΙ with an IC ₅₀ of 8.3 μM, has antitumor activity.

IC50 & Target

Kd: 5.85 μM (ezrin) ^[1]
IC50: 8.3 μM (ezrin) ^[1]

In Vitro

NSC305787 is an inhibitor of ezrin with a K _d of 5.85 μM, and has antitumor activity. NSC305787 inhibits PKCΙ phosphorylation of Ezrin, Moesin, Radixin, MBP, with IC ₅₀ s of 8.3, 9.4, 55, 58.9 μM, respectively. NSC305787 binds to PKCΙ with a K _d 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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

NSC305787 (0.240 mg/kg/day, i.p.) suppresses ezrin-dependent osteosarcoma metastatic growth in mouse lung ^[1] . NSC305787 (240 μg/kg, i.p.) dramatically inhibits pulmonary metastasis in a transgenic mouse model of osteosarcoma (Osx-Cre ⁺ p53 ^fl/fl pRB ^fl/fl ) and shows a more favorable pharmacokinetic profile compared with NSC668394 in the mouse model ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 6 mg/mL ( 13.47 mM ; Need ultrasonic and warming)

Preparing
Stock Solutions

Concentration Solvent Mass	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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

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

Solubility: ≥ 0.6 mg/mL (1.35 mM); Clear solution
2.

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

Solubility: ≥ 0.6 mg/mL (1.35 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 0.6 mg/mL (1.35 mM); Clear solution

* All of the co-solvents are available by MCE.