Danusertib (PHA739358)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1180 | Check With Us |
| 500mg | $1790 | Check With Us |
| 1g | $2685 | Check With Us |
: Cat #: V0348 CAS #: 827318-97-8 Purity ≥ 98%
Description: Danusertib (formerly PHA-739358), a pyrrolo-pyrazole compound, is a potent Aurora kinase inhibitor of Aurora A/B/C with potential antitumor activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 474.55 |
|---|---|
| Molecular Formula | C26H30N6O3 |
| CAS No. | 827318-97-8 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 95 mg/mL (200.2 mM)r |
| Water:<1 mg/mL (slightly soluble or insoluble)r | |
| Ethanol: <1 mg/mL (slightly soluble or insoluble) | |
| Solubility In Vivo | 1% DMSO+30% polyethylene glycol+1% Tween 80: 30mg/mL |
| SMILES Code | O=C(NC1=NNC2=C1CN(C([C@H](OC)C3=CC=CC=C3)=O)C2)C4=CC=C(N5CCN(C)CC5)C=C4 |
| Synonyms | PHA739358; PHA-739358; PHA 739358; Danusertib |
| Protocol | In Vitro | Danusertib (0.01 to 50 μM) significantly decreases viability of C13 and A2780cp cells. The IC50s are 10.40 and 1.83 μM for C13 cells, and 19.89 and 3.88 μM for A2780cp cells after 24- and 48-h treatment. Danusertib induces cell cycle arrest in G2/M phase in C13 and A2780cp cells. Danusertib treatment results in a marked increase in the percentage of cells arrested in G2/M phase and an accumulation of polyploidy in C13 and A2780cp cells. Danusertib demotes the expression of CDK1/CDC2 and cyclin B1 but promotes the expression of p21 Waf1/Cip1, p27 Kip1, and p53. Danusertib induces autophagy in C13 and A2780cp cells with the involvement of PI3K/Akt/mTOR signaling pathway. |
|---|---|---|
| In Vivo | PHA-739358 (15 mg/kg twice a day, i.p.) and IM are well tolerated, and significantly inhibit proliferation of K562 cells andvirtually suppressed tumor growth during the 10-day treatment period. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.1073 mL | 10.5363 mL | 21.0726 mL | 42.1452 mL |
| 5mM | 0.4215 mL | 2.1073 mL | 4.2145 mL | 8.4290 mL |
| 10mM | 0.2107 mL | 1.0536 mL | 2.1073 mL | 4.2145 mL |
| 20mM | 0.1054 mL | 0.5268 mL | 1.0536 mL | 2.1073 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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Concentration
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Volume
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Molecular Weight*
The dilution calculator equation
Concentration(start)
×
Volume(start)
=
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Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
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V1
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C2
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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.