1. Protein Tyrosine Kinase/RTK
    Cell Cycle/DNA Damage
    Apoptosis
  2. c-Kit
    PDGFR
    RAD51
    FLT3
    c-Met/HGFR
    RET
    Apoptosis
  3. Amuvatinib

Amuvatinib (Synonyms: MP470; HPK 56)

Cat. No.: HY-10206 Purity: 99.36%
Handling Instructions

Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair. Antineoplastic activity.

For research use only. We do not sell to patients.

Amuvatinib Chemical Structure

Amuvatinib Chemical Structure

CAS No. : 850879-09-3

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10 mM * 1 mL in DMSO USD 121 In-stock
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10 mg USD 180 In-stock
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50 mg USD 540 In-stock
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100 mg USD 950 In-stock
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Description

Amuvatinib (MP470) is an orally bioavailable multi-targeted tyrosine kinase inhibitor with potent activity against mutant c-Kit, PDGFRα, Flt3, c-Met and c-Ret. Amuvatinib (MP470) is also a DNA repair suppressor through suppression of DNA repair protein RAD51, thereby disrupting DNA damage repair[1][2][3]. Antineoplastic activity[4].

IC50 & Target

PDGFRαV561D

40 nM (IC50)

PDGFRαD842V

81 nM (IC50)

c-KitD816H

10 nM (IC50)

c-KitV560G

34 nM (IC50)

c-KitV654A

127 nM (IC50)

c-KitD816V

950 nM (IC50)

In Vitro

Amuvatinib (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[4].
Amuvatinib (MP470), a novel receptor tyrosine kinase (RTK) inhibitor has shown growth inhibitory activity against a variety of cancer cell lines. Amuvatinib (0.1-10 μM, 4 days incubation) is effective on LNCaP and PC-3 cells with IC50s of ~4 μM and 8 μM, respectively. When Erlotinib (10 μM) is combined with varying doses of Amuvatinib, the IC50 of Amuvatinib decreases to 2 μM on LNCaP cells[5].
Akt activity (as measured by phosphorylation on Ser473) is significantly reduced by 10 μM Amuvatinib (treated for 30 hours) alone but is not reduced by Erlotinib or Imatinib Mesylate (IM). Moreover, Amuvatinib plus Erlotinib completely abolished Akt phosphorylation in LNCaP cells with an unchanged total protein level of Akt[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: Prostate cancer cell lines (LNCaP, PC-3 and DU-145)
Concentration: 0.1-10 μM
Incubation Time: 4 days
Result: The IC50 for LNCaP and PC-3 was ~4 μM and 8 μM, respectively. Had only a modest effect on the viability of DU-145 cells.

Western Blot Analysis[2]

Cell Line: LNCaP cells
Concentration: 2,5,10 μM
Incubation Time: 30 hours
Result: Akt activity (as measured by phosphorylation on Ser473) was significantly reduced at 10 μM.
In Vivo

Four 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)[5].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Forty eight 6-7 week-old SCID male mice with LNCaP xenograft model[2]
Dosage: 10 mg/kg and 20 mg/kg, 50 mg/kg
Administration: Administered i.p. daily from days 1 to 24
Result: Individual therapy showed modest tumor growth inhibition (TGI), while combination had a marked effect on TGI (45-65%).
Clinical Trial
Molecular Weight

447.51

Formula

C₂₃H₂₁N₅O₃S

CAS No.

850879-09-3

SMILES

S=C(N1CCN(C2=C3OC4=CC=CC=C4C3=NC=N2)CC1)NCC5=CC=C6OCOC6=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (111.73 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2346 mL 11.1729 mL 22.3459 mL
5 mM 0.4469 mL 2.2346 mL 4.4692 mL
10 mM 0.2235 mL 1.1173 mL 2.2346 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.59 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

AmuvatinibMP470 HPK 56MP 470MP-470HPK56HPK 56HPK-56c-KitPDGFRRAD51FLT3c-Met/HGFRRETApoptosisSCFRCD117Platelet-derived growth factor receptorCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Inhibitorinhibitorinhibit

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Amuvatinib
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