2. Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. Trk Receptor
  4. PF-06273340

PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain.

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

PF-06273340

PF-06273340 Chemical Structure

CAS No. : 1402438-74-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

PF-06273340 Related Antibodies

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TrkA TrkB TrkC Trk

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Description

PF-06273340 is a peripherally restricted pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, and TrkC receptors. PF-06273340 binds in a DFG-out conformation, targeting less conserved kinase ligand binding domain regions outside the ATP binding pocket. PF-06273340 exhibits anti-hyperalgesic and analgesic effects. PF-06273340 can be used for the research of pain[1][2].

IC50 & Target[1]

TrkC

3 nM (IC50)

TrkB

4 nM (IC50)

TrkA

6 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HepG2 IC50
> 300 μM
Compound: 14; PF-06273340
Toxicity in human HepG2 cells
Toxicity in human HepG2 cells
[PMID: 27766865]
In Vitro

PF-06273340 potently inhibits TrkA, TrkB, and TrkC kinases with IC50 values of 6 nM, 4 nM, and 3 nM, respectively[1].
PF-06273340 exhibits low metabolic turnover in human liver microsomes, with a rate of <8.0 μL/min/mg protein[1].
PF-06273340 is a good substrate for P-glycoprotein, as demonstrated by an efflux ratio of 35.7 in the MDCK-MDR1 assay[1].
PF-06273340 is a substrate for BCRP, as demonstrated by an efflux ratio of 4.0[1].
PF-06273340 (1 μM) is highly kinase-selective, potently inhibiting only MUSK (IC50 = 53 nM), FLT-3 (IC50 = 395 nM), IRAK1 (IC50 = 2.5 μM), MKK (90% at 1 μM), and DDR1 (60% at 1 μM) among 309 tested kinases[1].
PF-06273340 has no measurable activity at the hERG channel, with an IC50 >30.0 μM[1].
PF-06273340 exhibits minimal cytotoxicity in THLE cells (IC50 >42 μM) and HepG2 cells (IC50 >300 μM)[1].

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

PF-06273340 Related Antibodies
Clinical Trial
Molecular Weight

479.92

Formula

C23H22ClN7O3
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(NC1=CC(C(C2=CN(C(C)(C)CO)C3=NC(N)=NC=C32)=O)=CN=C1)CC4=NC=C(Cl)C=C4
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 : 20 mg/mL (41.67 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0837 mL 10.4184 mL 20.8368 mL
5 mM 0.4167 mL 2.0837 mL 4.1674 mL
View the Complete Stock Solution Preparation Table

* 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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.8%

SDS (392 KB)

COA (250 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0837 mL 10.4184 mL 20.8368 mL 52.0920 mL
5 mM 0.4167 mL 2.0837 mL 4.1674 mL 10.4184 mL
10 mM 0.2084 mL 1.0418 mL 2.0837 mL 5.2092 mL
15 mM 0.1389 mL 0.6946 mL 1.3891 mL 3.4728 mL
20 mM 0.1042 mL 0.5209 mL 1.0418 mL 2.6046 mL
25 mM 0.0833 mL 0.4167 mL 0.8335 mL 2.0837 mL
30 mM 0.0695 mL 0.3473 mL 0.6946 mL 1.7364 mL
40 mM 0.0521 mL 0.2605 mL 0.5209 mL 1.3023 mL
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PF-06273340 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PF-062733401402438-74-7PF06273340PF 06273340Trk ReceptorTropomyosin related kinase receptorinflammatory painP-glycoproteinTrkANGFhuman hepatocytesTrkBBCRPpan-Trk inhibitorhuman liver microsomesTrkCInhibitorinhibitorinhibit

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