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SCH772984 HCl
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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
SCH772984 HCl
😃Good
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
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $95 | Backorder | |
| 5 mg | $135 | Backorder | |
| 10 mg | $198 | Backorder |
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Product Introduction
Bioactivity
Chemical Properties
| 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 |
| Targets&IC50 | ERK2:1 nM, ERK1:4 nM |
| 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]. |
| Molecular Weight | 624.14 |
| Formula | C33H34ClN9O2 |
| Smiles | O=C(NC1=CC2=C(NN=C2C3=CC=NC=C3)C=C1)[C@H]4CN(CC(N5CCN(C6=CC=C(C7=NC=CC=N7)C=C6)CC5)=O)CC4.[H]Cl |
| Relative Density. | no data available |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | H2O: 23.5 mg/mL (with gentle warming) |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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