PF-4989216
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 | $980 | Check With Us |
| 500mg | $1420 | Check With Us |
| 1g | $2130 | Check With Us |
: Cat #: V0151 CAS #: 1276553-09-3 Purity ≥ 98%
Description: PF-4989216 is a novel, potent, orally bioactive and selective small molecule inhibitor of PI3K (phosphatidylinositol 3-kinase) with potential anticancer activity.
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- Physicochemical and Storage Information
- Protocol
- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 380.40 |
|---|---|
| Molecular Formula | C18H13FN6OS |
| CAS No. | 1276553-09-3 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 76 mg/mL (199.8 mM)r |
| Water:<1 mg/mLr | |
| Ethanol: 7 mg/mL warming (18.4 mM | |
| Solubility In Vivo | Suspended in 0.5% methylcellulose: 1mg/mL |
| SMILES Code | N#CC1=C(N2CCOCC2)SC(C3=NC=NN3)=C1C4=CC=C(C#N)C=C4F |
| Synonyms | PF4989216; PF 4989216; PF-498921 |
| Protocol | In Vitro | PF-4989216 (Compound 10) has excellent PI3Kα Ki (0.6 nM), good cellular potency (S473 IC50=79 nM), and good selectivity against mTOR (mTOR Ki=1440 nM). PF-4989216 has PI3Kα Ki less than 1 nM and mTOR Ki more than 1 μM. PF-4989216 also has excellent selectivity over 40 other kinases, and no major CYP inhibitions are observed. Less than 30% inhibition is observed in 1A2, 2C9, 2D6, and 3A4 CYP enzymes at 3 μM. |
|---|---|---|
| In Vivo | PF-4989216 (Compound 10) is dosed orally in our in vivo antitumor model, PI3K driven NCI-H1975 xenograft tumors. PF-4989216 demonstrates dose responsive tumor growth inhibitory activity from 25 to 200 mg/kg in QD oral dosing. |
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 | 2.6288 mL | 13.1441 mL | 26.2881 mL | 52.5762 mL |
| 5mM | 0.5258 mL | 2.6288 mL | 5.2576 mL | 10.5152 mL |
| 10mM | 0.2629 mL | 1.3144 mL | 2.6288 mL | 5.2576 mL |
| 20mM | 0.1314 mL | 0.6572 mL | 1.3144 mL | 2.6288 mL |
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
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Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
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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.