SCH772984

This product is for research use only, not for human use. We do not sell to patients.

SCH772984
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250mg$1220Check With Us
500mg$1950Check With Us
1g$2925Check With Us

Cat #: V0463 CAS #: 942183-80-4 Purity ≥ 98%

Description: SCH772984 (SCH-772984) is a novel, potent and ATP-competitive inhibitor of ERK1/2 with potential antitumor activity.

References: Morris EJ, et al. Discovery of a novel ERK inhibitor with activity in models of acquired resistance to BRAF and MEK inhibitors. Cancer Discov. 2013 Jul;3(7):742-50.

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Molecular Weight (MW)587.67
Molecular FormulaC33H33N9O2
CAS No.942183-80-4
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 0.1 mg/mL (0.17 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
Solubility In Vivo5% DMSO+30% PEG 300+ddH2O: 0.6 mg/mL
SMILES CodeO=C([C@H]1CN(CC(N2CCN(C3=CC=C(C4=NC=CC=N4)C=C3)CC2)=O)CC1)NC5=CC6=C(NN=C6C7=CC=NC=C7)C=C5
SynonymsSCH-772984; SCH 772984; SCH772984;
ProtocolIn VitroSCH772984 shows EC50 values less than 500 nM in approximately 88% and 49% of BRAF-mutant (n=25) or RAS-mutant (n=35) tumor lines, respectively. SCH772984 (3-300 nM; 24 hours) inhibits ERK and RSK phosphorylation. SCH772984 (300 nM; 24-48hours) results in a G1 arrest in SCH772984-sensitive melanoma cells.
In VivoDose-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. SCH772984 is well tolerated on this schedule as measured by morbidity, lethality, or body weight loss. SCH772984 (12.5-50 mg/kg; i.p.; twice daily for 14 days) leads to 98% tumor regression.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.7016 mL8.5082 mL17.0164 mL34.0327 mL
5mM0.3403 mL1.7016 mL3.4033 mL6.8065 mL
10mM0.1702 mL0.8508 mL1.7016 mL3.4033 mL
20mM0.0851 mL0.4254 mL0.8508 mL1.7016 mL
Quality Control Documentation
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

This equation is commonly abbreviated as: C1 V1 = C2 V2

Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
Step One: Enter information below
Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals
Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

Calculation Results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid 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 master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (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.