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SCH772984 HCl

SCH772984 HCl
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SCH772984 HCl

Catalog No. T23337
SCH772984 HCl is a selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors, with IC50s of 4 and 1 nM, respectively. SCH772984 HCl has nanomolar cellular potency in tumor cells with mutations in BRAF, NRAS, or KRA
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Pack SizePriceAvailabilityQuantity
2 mg$95Backorder
5 mg$135Backorder
10 mg$198Backorder
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Product Introduction

Bioactivity
Description
SCH772984 HCl is a selective inhibitor of ERK1/2 that displays behaviors of both type I and type II kinase inhibitors, with IC50s of 4 and 1 nM, respectively. SCH772984 HCl has nanomolar cellular potency in tumor cells with mutations in BRAF, NRAS, or KRA
In vitro
In LOX BRAFV600E melanoma cells, SCH772984 HCl (3, 10, 30, 100, 300 nM; 24 hours) inhibited ERK and RSK phosphorylation. SCH772984 HCl showed EC50 values less than 500 nM in approximately 88% and 49% of BRAF-mutant (n=25) or RAS-mutant (n=35) tumor lines, respectively. In SCH772984 HCl-sensitive melanoma cells, SCH772984 HCl (300 nM; 24-48hours) resulted in a G1 arrest[1].
In vivo
In female nude mice bearing human LOX BRAFV600E tumors, SCH772984 HCl (12.5, 25, 50 mg/kg; i.p. twice daily for 14 days) lead to 98% tumor regression at all doses. Dose-dependent antitumor activity is also observed in the KRAS-mutant pancreatic MiaPaCa model, with 36% regression at 50 mg/kg twice daily. Importantly, tumor regression is accompanied by robust inhibition of ERK phosphorylation in tumor tissue[1].
Chemical Properties
Molecular Weight624.14
FormulaC33H34ClN9O2
Cas No.
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility Information
H2O: 23.5mg/mL (with gentle warming)

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