Art. -Nr.: HY-131972

PF-06843195

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PF-06843195 is a highly selective PI3Kα inhibitor with an IC₅₀ of 18 nM in Rat1 fibroblasts. The K_is 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.

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Reinheit: 98.12%
CAS. Nr.: 2067281-51-8
Formel: C₂₀H₂₅F₃N₈O₄
Molecular Weight:498.46

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

PF-06843195 Chemical Structure

CAS. Nr.: 2067281-51-8

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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)

Alle PI3K Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
MCF7	IC₅₀	62 nM Compound: 1; PF-06843195	Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 7 days by Cell-titer Glo reagent based assay Antiproliferation activity against human MCF7 cells assessed as reduction in cell viability incubated for 7 days by Cell-titer Glo reagent based assay	[PMID: 33356246]
T47D	IC₅₀	32 nM Compound: 1; PF-06843195	Antiproliferation activity against human T47D cells assessed as reduction in cell viability incubated for 7 days by Cell-titer Glo reagent based assay Antiproliferation activity against human T47D cells assessed as reduction in cell viability incubated for 7 days by Cell-titer Glo reagent based assay	[PMID: 33356246]

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].

MedChemExpress (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].

MedChemExpress (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:

T_1/2 of 3.6 h for rats.

Chemical Information

CAS. Nr. 2067281-51-8
Appearance Solid
Molecular Weight 498.46
Formel C₂₀H₂₅F₃N₈O₄
Color White to off-white
SMILES

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

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 60 mg/mL (120.37 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hengmiao Cheng, et al. Structure-Based Drug Design and Synthesis of PI3Kα-Selective Inhibitor (PF-06843195). J Med Chem. 2021 Jan 14;64(1):644-661. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.0062 mL	10.0309 mL	20.0618 mL	50.1545 mL
	5 mM	0.4012 mL	2.0062 mL	4.0124 mL	10.0309 mL
	10 mM	0.2006 mL	1.0031 mL	2.0062 mL	5.0154 mL
	15 mM	0.1337 mL	0.6687 mL	1.3375 mL	3.3436 mL
	20 mM	0.1003 mL	0.5015 mL	1.0031 mL	2.5077 mL
	25 mM	0.0802 mL	0.4012 mL	0.8025 mL	2.0062 mL
	30 mM	0.0669 mL	0.3344 mL	0.6687 mL	1.6718 mL
	40 mM	0.0502 mL	0.2508 mL	0.5015 mL	1.2539 mL
	50 mM	0.0401 mL	0.2006 mL	0.4012 mL	1.0031 mL
	60 mM	0.0334 mL	0.1672 mL	0.3344 mL	0.8359 mL
	80 mM	0.0251 mL	0.1254 mL	0.2508 mL	0.6269 mL
	100 mM	0.0201 mL	0.1003 mL	0.2006 mL	0.5015 mL

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PF-06843195

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Alle PI3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

PF-06843195 Related Classifications

HY-131972 Related Classifications