Nirogacestat (PF-03084014; PF-3084014)
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 | $1450 | Check With Us |
| 500mg | $2250 | Check With Us |
| 1g | $3375 | Check With Us |
: Cat #: V0723 CAS #: 1290543-63-3 Purity ≥ 98%
Description: Nirogacestat (formerly also known as PF-03084014; PF03084014; PF 3084014; PF-3084014) is an orally bioavailable, reversible, noncompetitive, and selective γ-secretase/gamma secretase (GS) inhibitor with potential anticancer activity.
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- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 489.64 |
|---|---|
| Molecular Formula | C27H41F2N5O |
| CAS No. | 1290543-63-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 97 mg/mL (198.1 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 97 mg/mL (198.1 mM) | |
| SMILES Code | CCC[C@H](N[C@@H]1CC2=C(C=C(F)C=C2F)CC1)C(NC3=CN(C(C)(C)CNCC(C)(C)C)C=N3)=O |
| Synonyms | PF 03084014; PF-3084014; Nirogacestat, PF03084014; PF-03084014; PF3084014; PF 3084014 |
| Protocol | In Vitro | The IC50 of Nirogacestat (PF-03084014) for γ-secretase enzyme inhibition in cell-free assay for Aβ production using detergent solubilized membranes derived from HeLa cells is determined to be 6.2 nM. When tested for inhibition of Notch receptor cleavage in cellular assays using HPB-ALL cells that harbor mutations in both the heterodimerization and PEST domains in Notch1, the cell IC50 is determined to be 13.3 nM. Nirogacestat (PF-03084014) causes a significant increase in caspase-3 activities in HPB-ALL and TALL-1 cells as well as an induction of cleaved PARP and cleaved caspase-3 after a 7-day treatment. |
|---|---|---|
| In Vivo | Nirogacestat (PF-03084014) shows robust antitumor activity in this model on 14-day twice daily dosing. Tumor growth inhibition is dose dependent, with maximal tumor growth inhibition of ~92% obtained at high dose levels (150 mg/kg). In tumor growth inhibition studies where mice receive repetitive twice daily dosing for more than a week, Nirogacestat (PF-03084014) is well tolerated at dose levels below 100 mg/kg as no significant weight loss, morbidity, or mortality is observed. When the dose is increased to 150 mg/kg, however, mice have diarrhea and show weight loss (10-15%) approximately 10 days after compound administration. The body weight of treated animals usually returns to normal if dosing holidays are given, suggesting that the toxicity of Nirogacestat (PF-03084014) is reversible. |
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 | 2.0423 mL | 10.2116 mL | 20.4232 mL | 40.8463 mL |
| 5mM | 0.4085 mL | 2.0423 mL | 4.0846 mL | 8.1693 mL |
| 10mM | 0.2042 mL | 1.0212 mL | 2.0423 mL | 4.0846 mL |
| 20mM | 0.1021 mL | 0.5106 mL | 1.0212 mL | 2.0423 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
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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
×
Volume(start)
V1
=
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C2
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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.