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

PF-06843195 

Cat. No.: HY-131972
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

Size Price Stock
5 mg USD 500 Ask For Quote & Lead Time
10 mg USD 850 Ask For Quote & Lead Time
25 mg USD 1800 Ask For Quote & Lead Time
50 mg USD 3100 Ask For Quote & Lead Time
100 mg USD 4700 Ask For Quote & Lead Time

* Please select Quantity before adding items.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PF-06843195
Cat. No.:
HY-131972
Quantity:
MCE Japan Authorized Agent: