PF-04691502
This product is for research use only, not for human use. We do not sell to patients.
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| Size | Price | Stock |
|---|---|---|
| 250mg | $850 | Check With Us |
| 500mg | $1450 | Check With Us |
| 1g | $2175 | Check With Us |
: Cat #: V0123 CAS #: 1013101-36-4 Purity ≥ 98%
Description: PF-04691502 is a novel, potent, ATP-competitive and selective dual inhibitor of PI3K (phosphatidylinositol 3 kinase) and mTOR (mammalian target of rapamycin) with potential anticancer activity.
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| Molecular Weight (MW) | 425.48 |
|---|---|
| Molecular Formula | C22H27N5O4 |
| CAS No. | 1013101-36-4 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 14 mg/mL (32.9 mM)r |
| Water:<1 mg/mLr | |
| Ethanol: <1 mg/mL | |
| SMILES Code | O=C1C(C2=CC=C(OC)N=C2)=CC3=C(C)N=C(N)N=C3N1[C@H]4CC[C@H](OCCO)CC4 |
| Synonyms | PF-04691502; PF 04691502; PF04691502; PF 4691502; PF4691502; PF-4691502 |
| Protocol | In Vitro | PF-04691502 inhibits recombinant mouse PI3Kα in an ATP-competitive inhibitor. PF-04691502 potently inhibits AKT phosphorylation on S473 and T308 in all the 3 cancer cell lines with IC50 values of 3.8 to 20 nM and 7.5 to 47 nM, respectively. Using a 96-well plate-based P-S6RP(S235/236) ELISA assay, PF-04691502 potently inhibits mTORC1 activity with an IC50 of 32 nM. PF-04691502 inhibits cell proliferation of BT20, SKOV3, and U87MG with IC50 values of 313, 188, and 179 nM, respectively. In PIK3CA-mutant and PTEN-deleted cancer cell lines, PF-04691502 reduces phosphorylation of AKT T308 and AKT S473 (IC50 of 7.5-47 nM and 3.8-20 nM, respectively) and inhibits cell proliferation (IC50 of 179-313 nM). PF-04691502 inhibits mTORC1 activity in cells as measured by PI3K-independent nutrient stimulated assay, with an IC50 of 32 nM and inhibits the activation of PI3K and mTOR downstream effectors including AKT, FKHRL1, PRAS40, p70S6K, 4EBP1, and S6RP. |
|---|---|---|
| In Vivo | Nude mice bearing U87MG tumors are administered orally once a day with PF-04691502 at 0.5, 1, 5, and 10 mg/kg (maximum tolerated dose, MTD). Treatment with 10 mg/kg results in a significant reduction of P-AKT(S473) levels at 1 hour postdosing, and persistent inhibition is observed for 8 hours. P-AKT(S473) recovers to above baseline 24 hours after 10 mg/kg treatment. For P-S6RP(S235/236), a similar inhibition time course is observed, but after 24 hours of treatment, P-S6RP levels remain lower than vehicle tumors. Modulation of the AKT downstream effector, P-PRAS40(T246), and mTOR downstream effector, P-4EBP1(T37/46), is observed. The PF-04691502-treated tumors are also evaluated by immunohistochemistry for levels of P-AKT(S473), total AKT, P-S6RP, and total S6RP. Phosphorylation of AKT and S6RP are significantly reduced at 4 hours after a single dose of PF-04691502 at 10 mg/kg. Dose-dependent tumor growth inhibition (TGI) is obtained in the U87MG xenograft model and approximately 73% TGI is observed at the MTD dose of 10 mg/kg. |
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 | 2.3503 mL | 11.7514 mL | 23.5029 mL | 47.0057 mL |
| 5mM | 0.4701 mL | 2.3503 mL | 4.7006 mL | 9.4011 mL |
| 10mM | 0.2350 mL | 1.1751 mL | 2.3503 mL | 4.7006 mL |
| 20mM | 0.1175 mL | 0.5876 mL | 1.1751 mL | 2.3503 mL |
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