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NSC305787 hydrochloride

Catalog No. T12263L   CAS 53868-26-1
Synonyms: (Rac)-NSC305787 hydrochloride

NSC305787 hydrochloride ((Rac)-NSC305787 hydrochloride is a cell membrane permeable and selective and potent small molecule dual inhibitor of Cdc25 dual specificity phosphatase and EZR that displays antitumor activity in pancreatic cancer cells and inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.NSC 663284 inhibits NSD2 (IC50 of 170 nM) enzyme activity.

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NSC305787 hydrochloride Chemical Structure
NSC305787 hydrochloride, CAS 53868-26-1
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Purity: 99.07%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description NSC305787 hydrochloride ((Rac)-NSC305787 hydrochloride is a cell membrane permeable and selective and potent small molecule dual inhibitor of Cdc25 dual specificity phosphatase and EZR that displays antitumor activity in pancreatic cancer cells and inhibits Cdc25B2, Cdc25A, Cdc25B2 and Cdc25C.NSC 663284 inhibits NSD2 (IC50 of 170 nM) enzyme activity.
Targets&IC50 Ezrin:8.3 μM, Radixin:55 μM, PKCΙ:172.4 μM (Kd), MBP:58.9 μM, Ezrin:5.85 μM (Kd), Moesin:9.4 μM
In vitro NSC305787 hydrochloride, an inhibitor of ezrin, exhibits a Kd of 5.85 μM and demonstrates antitumor activity. With IC50 values of 8.3, 9.4, 55, and 58.9 μM, NSC305787 hydrochloride inhibits PKCΙ phosphorylation of Ezrin, Moesin, Radixin, and MBP, respectively. Binding to PKCΙ with a Kd value of 172.4 μM, NSC305787 hydrochloride primarily inhibits ezrin T567 phosphorylation through its binding to ezrin, not via the inhibition of PKCΙ kinase activity. In the context of K7M2 osteosarcoma (OS) cells, NSC305787 hydrochloride (1, 10 μM) displays inhibitory activity against ezrin-mediated invasion. Furthermore, at a concentration of 10 μM, NSC305787 hydrochloride diminishes cell motility phenotypes in zebrafish and hinders OS metastatic growth in lung organ culture[2].
In vivo In a mouse model,NSC305787 hydrochloride (i.p., 0.240 mg/kg/day) effectively suppresses ezrin-dependent osteosarcoma metastatic growth in the lung[1]. Additionally, in a transgenic mouse model of osteosarcoma (Osx-Cre+p53fl/flpRBfl/fl), NSC305787 hydrochloride (i.p., 240 μg/kg) exhibits a remarkable inhibition of pulmonary metastasis. Furthermore, it demonstrates a more favorable pharmacokinetic profile compared to NSC668394 in the same mouse model[1].
Synonyms (Rac)-NSC305787 hydrochloride
Molecular Weight 481.89
Formula C25H31Cl3N2O
CAS No. 53868-26-1

Storage

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 5 mg/mL(10.38 mM), Sonification is recommended.

H2O: <0.1 mg/mL(Insoluble)

TargetMolReferences and Literature

1. Çelik H, et al. Ezrin Inhibition Up-regulates Stress Response Gene Expression. J Biol Chem. 2016 Jun 17;291(25):13257-70. 2. Bulut G, et al. Small molecule inhibitors of ezrin inhibit the invasive phenotype of osteosarcoma cells. Oncogene. 2012 Jan 19;31(3):269-81.

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Keywords

NSC305787 hydrochloride 53868-26-1 Others (Rac)-NSC305787 hydrochloride NSC305787 Hydrochloride NSC-305787 Hydrochloride NSC-305787 hydrochloride NSC 305787 Hydrochloride inhibitor inhibit

 

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