GNF-5837
| Code | Size | Price |
|---|
| SYN-1183-M100 | 100 mg | Enquire |
Quantity:
| SYN-1183-M001 | 1 mg | £104.00 |
Quantity:
| SYN-1183-M005 | 5 mg | £162.00 |
Quantity:
| SYN-1183-M010 | 10 mg | £244.00 |
Quantity:
| SYN-1183-M050 | 50 mg | £848.00 |
Quantity:
Prices exclude any Taxes / VAT
Overview
Regulatory Status: RUO
Shipping:
-20°C
Documents
Further Information
Alternate Names/Synonyms:
GNF5837
Appearance:
Solid.
CAS:
1033769-28-6
EClass:
32160000
Form (Short):
liquid
InChi:
InChI=1S/C28H21F4N5O2/c1-15-4-6-19(35-27(39)37-25-11-16(28(30,31)32)5-9-22(25)29)13-23(15)34-18-7-8-20-21(12-17-3-2-10-33-17)26(38)36-24(20)14-18/h2-14,33-34H,1H3,(H,36,38)(H2,35,37,39)/b21-12-
InChiKey:
YYDUWLSETXNJJT-MTJSOVHGSA-N
Long Description:
Chemical. CAS: 1033769-28-6. Formula: C28H21F4N5O2. MW: 535.5. Inhibitor of pan-Trk activity (IC(50) = 8 and 12nM 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 (IC(50) = 11, 9 and 7nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC(50) = 42 and 17nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC(50) = 1 and 0.5µM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC(50) = 3.0 and 5.6µM). Displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. Weakly active against relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. Suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50mg/kg, p.o.).
Molecular Formula:
C28H21F4N5O2
Molecular Weight:
535.5
Package Type:
Plastic Vial
Product Description:
Inhibitor of pan-Trk activity (IC(50) = 8 and 12nM 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 (IC(50) = 11, 9 and 7nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC(50) = 42 and 17nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC(50) = 1 and 0.5µM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC(50) = 3.0 and 5.6µM). Displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. Weakly active against relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. Suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50mg/kg, p.o.).
Purity:
>95%
Solubility Chemicals:
Soluble in DMSO.
Transportation:
Non-hazardous
UNSPSC Category:
Protein Kinase Modulators
UNSPSC Number:
12352200
Use & Stability:
Stable for at least 2 years after receipt when stored at -20°C.
References
Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models: P. Albaugh, et al.; ACS Med. Chem. Lett. 3, 140 (2012)
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