Home Protein Tyrosine Kinase Trk receptor inhibitor PF-06273340 For research use only.

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 No. 1402438-74-7

Purity & Quality Control

PF-06273340 Related Products

Signaling Pathway

Trk receptor Signaling Pathways

Trk receptor Signaling Pathway

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


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In vivo
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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. )

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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

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