PF-06273340

PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.

PF-06273340 Chemical Structure

PF-06273340 Chemical Structure

CAS: 1402438-74-7

Purity & Quality Control

Batch: Purity: 99.46%
99.46

PF-06273340 Related Products

Choose Selective Trk receptor Inhibitors

Biological Activity

Description PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively.
Targets
TrkC [1]
(Cell-free assay)
TrkB [1]
(Cell-free assay)
TrkA [1]
(Cell-free assay)
3 nM 4 nM 6 nM
In vitro
In vitro PF-06273340 is a highly potent pan-Trk inhibitor, with an excellent LipE profile. PF-06273340 is profiled in a series of in vitro safety assays, showing little cytotoxicity in THLE or HepG2 cell lines (IC50 > 42 μM and >300 μM, respectively). In this broad panel, all IC50/Ki values were >10 μM except for COX-1 (IC50 = 2.7 μM) and dopamine transporter assays (Ki = 5.2 μM) and PDEs 4D, 5A, 7B, 8B, and 11 (54−89% inhibition at 10 μM). PF-06273340 is screened in the Invitrogen wide kinase panel of 309 kinases, and all were inhibited by <40% when tested at 1 μM except the following: MUSK (IC50 53 nM), FLT-3 (IC50 395 nM), IRAK1 (IC50 2.5 μM), MKK (90% @ 1 μM), and DDR1 (60% @ 1 μM)[1].
In Vivo
In vivo In rats, decreases in white blood cell count are observed from 150 mg/kg/day. At doses ≥250 mg/kg, increases in body weight gain and food consumption are observed, effects that could be rationalized as being mediated by central inhibition of TrkB, agonists of which are known to be anorexigenic in rodents. Adaptive changes in the liver are observed microscopically and accompanied by increased liver weight at ≥250 mg/kg and increases cholesterol at 1000 mg/kg. Overall, PF-06273340 is well tolerated up to 1000 mg/kg/day where plasma exposure (unbound Cavg) is approximately 400×TrkA IC50[1].
Animal Research Animal Models Male SD rats
Dosages 0.25, 2.5 and 25 mg/kg
Administration oral administration

Chemical Information & Solubility

Molecular Weight 479.92 Formula

C23H22ClN7O3

CAS No. 1402438-74-7 SDF Download PF-06273340 SDF
Smiles CC(C)(CO)N1C=C(C2=CN=C(N=C21)N)C(=O)C3=CC(=CN=C3)NC(=O)CC4=NC=C(C=C4)Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 95 mg/mL ( (197.94 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 1 mg/mL

Water : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration 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 addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy PF-06273340 | PF-06273340 supplier | purchase PF-06273340 | PF-06273340 cost | PF-06273340 manufacturer | order PF-06273340 | PF-06273340 distributor