1. Protein Tyrosine Kinase/RTK
  2. Trk Receptor

GNF-5837 

Cat. No.: HY-13491 Purity: 99.01%
Handling Instructions

GNF-5837 is a potent pan-Trk inhibitor which display antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively).

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

GNF-5837 Chemical Structure

GNF-5837 Chemical Structure

CAS No. : 1033769-28-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 84 In-stock
Estimated Time of Arrival: December 31
10 mg USD 120 In-stock
Estimated Time of Arrival: December 31
50 mg USD 324 In-stock
Estimated Time of Arrival: December 31
100 mg USD 540 In-stock
Estimated Time of Arrival: December 31
200 mg USD 792 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

GNF-5837 is a potent pan-Trk inhibitor which display antiproliferative effects in cellular Ba/F3 assays (IC50 values are 7, 9 and 11 nM for cells containing the fusion proteins Tel-TrkC, Tel-TrkB and Tel-TrkA, respectively). IC50 Value: 7/9/11 nM (Tel-TrkC/Tel-TrkB/Tel-TrkA) [1] Target: pan-Trk GNF-5837 is an orally bioavailable oxindole compound that and acts as a potent, reversible and type II DFG-out inhibitor of pan-Trk activity (IC50 = 8 and 12 nM for TrkA and TrkB). Shown to target Trk (tropomyosin receptor kinase) ATP binding cleft and an immediately adjacent hydrophobic pocket. Preferentially arrests the proliferation of Ba/F3 cells fused with Tel-TrkA, Tel-TrkB and Tel-TrkC (IC50 = 11, 9 and 7 nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC50 = 42 and 17 nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC50 = 1 and 0.5 μM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC50 = 3.0 and 5.6 μM). GNF-5837 displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. GNF-5837 weakly antagonize relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. GNF-5837 suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50 mg/kg, p.o.) [1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 32 mg/mL (59.76 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8674 mL 9.3372 mL 18.6745 mL
5 mM 0.3735 mL 1.8674 mL 3.7349 mL
10 mM 0.1867 mL 0.9337 mL 1.8674 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

535.49

Formula

C₂₈H₂₁F₄N₅O₂

CAS No.

1033769-28-6

SMILES

O=C(NC1=CC(C(F)(F)F)=CC=C1F)NC2=CC=C(C)C(NC3=CC(NC/4=O)=C(C=C3)C4=C\C5=CC=CN5)=C2

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

Room temperature in continental US; may vary elsewhere

Purity: 99.01%

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Product Name:
GNF-5837
Cat. No.:
HY-13491
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GNF-5837

Cat. No.: HY-13491