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

Amuvatinib  (Synonyms: MP470; HPK 56)

Cat. No.: HY-10206 Purity: 99.47%
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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.

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Amuvatinib Chemical Structure

Amuvatinib Chemical Structure

CAS No. : 850879-09-3

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 133 In-stock
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10 mg USD 198 In-stock
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Based on 6 publication(s) in Google Scholar

Other Forms of Amuvatinib:

Amuvatinib Related Antibodies

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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].

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

Amuvatinib Related Antibodies

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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (111.73 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2346 mL 11.1729 mL 22.3459 mL 55.8647 mL
5 mM 0.4469 mL 2.2346 mL 4.4692 mL 11.1729 mL
10 mM 0.2235 mL 1.1173 mL 2.2346 mL 5.5865 mL
15 mM 0.1490 mL 0.7449 mL 1.4897 mL 3.7243 mL
20 mM 0.1117 mL 0.5586 mL 1.1173 mL 2.7932 mL
25 mM 0.0894 mL 0.4469 mL 0.8938 mL 2.2346 mL
30 mM 0.0745 mL 0.3724 mL 0.7449 mL 1.8622 mL
40 mM 0.0559 mL 0.2793 mL 0.5586 mL 1.3966 mL
50 mM 0.0447 mL 0.2235 mL 0.4469 mL 1.1173 mL
60 mM 0.0372 mL 0.1862 mL 0.3724 mL 0.9311 mL
80 mM 0.0279 mL 0.1397 mL 0.2793 mL 0.6983 mL
100 mM 0.0223 mL 0.1117 mL 0.2235 mL 0.5586 mL
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Amuvatinib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Amuvatinib850879-09-3MP470 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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