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Sapitinib (AZD-8931)

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

Sapitinib (AZD-8931)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
250mg$445In Stock
500mg$750In Stock
1g$1125In Stock

Cat #: V0567 CAS #: 848942-61-0 Purity ≥ 98%

Description: Sapitinib (formerly AZD8931; AZD-8931) is an orally bioactive, reversible and ATP competitive inhibitor of multiple kinases including EGFR, ErbB2/3 with potential antitumor activity.

References: Hickinson DM, et al. AZD8931, an equipotent, reversible inhibitor of signaling by epidermal growth factor receptor, ERBB2 (HER2), and ERBB3: a unique agent for simultaneous ERBB receptor blockade in cancer. Clin Cancer Res. 2010 Feb 15;16(4):1159-69.

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Molecular Weight (MW)473.93
Molecular FormulaC23H25ClFN5O3
CAS No.848942-61-0
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 40 mg/mL (84.4 mM)r
Water: <1 mg/mLr
Ethanol: <1 mg/mL
Solubility In Vivo30% PEG400+0.5% Tween80+5% propylene glycol: 5 mg/mL
SMILES CodeO=C(NC)CN1CCC(OC2=CC3=C(NC4=CC=CC(Cl)=C4F)N=CN=C3C=C2OC)CC1
SynonymsAZD 8931; Sapitinib; AZD 8931; AZD8931;
ProtocolIn VitroAZD8931 shows potent inhibitory effect on erbB2 in the ligand-independent MCF-7 cl24 cells, with IC50 of 59 nM.
In VivoAZD8931 (6.25-50 mg/kg, p.o.) significantly inhibits BT474c (breast), Calu-3 (NSCLC), LoVo (colorectal), FaDu (SCCHN), and PC-9 (NSCLC) tumor xenograft growth. AZD8931 is active in xenograft tumor models responsive to EGFR inhibition alone (LoVo and PC-9) or EGFR or erbB2 inhibition (BT474c, Calu-3, and FaDu). AZD8931 causes pharmacodynamic changes in proliferation and apoptosis markers in human tumor xenograft models.
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
1mM2.1100 mL10.5501 mL21.1002 mL42.2003 mL
5mM0.4220 mL2.1100 mL4.2200 mL8.4401 mL
10mM0.2110 mL1.0550 mL2.1100 mL4.2200 mL
20mM0.1055 mL0.5275 mL1.0550 mL2.1100 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.