1. PI3K/Akt/mTOR
  2. PI3K
  3. PF-06843195

PF-06843195 

Cat. No.: HY-131972 Purity: 99.06%
Handling Instructions

PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.

For research use only. We do not sell to patients.

PF-06843195 Chemical Structure

PF-06843195 Chemical Structure

CAS No. : 2067281-51-8

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5 mg USD 80 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy[1].

IC50 & Target[1]

PI3Kα

18 nM (IC50, in Rat1 fibroblasts)

PI3Kβ

360 nM (IC50, in Rat1 fibroblasts)

PI3Kδ

160 nM (IC50, in Rat1 fibroblasts)

PI3Kα

0.018 nM (Ki)

PI3Kδ

0.28 nM (Ki)

In Vitro

PF-06843195 inhibits the breast cancer cell lines MCF7 and T47D proliferation with IC50s of 62 nM and 32 nM, respectively[1].
PF-06843195 inhibits pAKT (T308) in MCF7 and T47D cells with IC50s of 7.8 nM and 8.7 nM, respectively[1].

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

In Vivo

In rats, PF-06843195 can rapidly and quantitatively transform from PF-06862309[1].
PF-06843195 exhibits oral bioavailability (rat 25 %) following oral administration (rat 10 mg/kg)[1].
PF-06843195 exhibits a moderate half-life (rat 3.6 h) due to high plasma clearance (30 mL/min/kg) combined with large volumes of distribution (3.0 L/kg) following intravenous administration (rat 2 mg/kg)[1].

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

Animal Model: Male Wistar Han Rats [1]
Dosage: 2 mg/kg (intravenous) and 10 mg/kg (oral gavage)(Pharmacokinetic Analysis)
Administration: Intravenous (IV) or oral gavage (PO)
Result: T1/2 of 3.6 h for rats.
Molecular Weight

498.46

Formula

C20H25F3N8O4

CAS No.
SMILES

OC[[email protected]]1(CN(CC1)C(OCC(F)F)=O)NC2=NC(N3CCOCC3)=NC(C4=CN=C(N)N=C4)=C2F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (125.39 mM; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0062 mL 10.0309 mL 20.0618 mL
5 mM 0.4012 mL 2.0062 mL 4.0124 mL
10 mM 0.2006 mL 1.0031 mL 2.0062 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.17 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.17 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Product Name:
PF-06843195
Cat. No.:
HY-131972
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