Amuvatinib (MP470; HPK56)

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

Amuvatinib (MP470; HPK56)
For small sizes, please check our retail website as below: www.invivochem.com
Size Price Stock
250mg$850Check With Us
500mg$1450Check With Us
1g$2175Check With Us

Cat #: V0579 CAS #: 850879-09-3 Purity ≥ 98%

Description: Amuvatinib (MP-470; HPK-56) is a novel, potent, orally bioavailable and multi-targeted inhibitor of c-Kit, PDGFRα and Flt3 with potential antineoplastic activity.

References: Choy G, et al. Safety, tolerability, and pharmacokinetics of amuvatinib from three phase 1 clinical studies in healthy volunteers. Cancer Chemother Pharmacol. 2012 Jul;70(1):183-90.

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Molecular Weight (MW)447.51
Molecular FormulaC23H21N5O3S
CAS No.850879-09-3
Storage-20℃ for 3 years in powder formr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: 32 mg/mL (71.5 mM)r
Water:<1 mg/mLr
Ethanol:<1 mg/mL
Solubility In Vivo30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL
SMILES CodeS=C(N1CCN(C2=C(OC3=CC=CC=C34)C4=NC=N2)CC1)NCC5=CC=C(OCO6)C6=C5
SynonymsAmuvatinib; MP470; HPK-56; MP-470; HPK 56; HPK56; MP 470;
ProtocolIn VitroAmuvatinib (MP470) inhibits c-Kit (D816V), c-Kit (D816H), c-Kit (V560G), c-Kit (V654A), PDGFRα (D842V), and PDGFRα (V561D) with IC50s of 950 nM, 10 nM, 34 nM, 127 nM, 81 nM, and 40 nM, respectively.
In VivoFour LNCaP xenograft arms each with 12 mice are dosed intraperitoneally with DMSO (control) or Erlotinib 80 mg/kg or Amuvatinib (MP470) 50 mg/kg or Erlotinib 80 mg/kg plus Amuvatinib 50 mg/kg daily for 2 weeks and then observed for a further 11 days. Individual therapy with Amuvatinib or Erlotinib shows modest tumor growth inhibition (TGI), while Amuvatinib plus Erlotinib has a marked effect on TGI (45-65%). However, due to the high doses of Amuvatinib used, only five or one mouse remained alive in the combination arm at the end of treatment or at the end of the study, respectively. Therefore the Amuvatinib dose is reduced to 10 mg/kg or 20 mg/kg for the combination treatment. TGI in the group receiving 10 mg/kg Amuvatinib+80 mg/kg Erlotinib is not significantly different from the control group. However, mice receiving 20 mg/kg Amuvatinib+80 mg/kg Erlotinib have a significant TGI compared to the control group (p=0.01).
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
1mM2.2346 mL11.1729 mL22.3459 mL44.6917 mL
5mM0.4469 mL2.2346 mL4.4692 mL8.9383 mL
10mM0.2235 mL1.1173 mL2.2346 mL4.4692 mL
20mM0.1117 mL0.5586 mL1.1173 mL2.2346 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.