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SynKinase
GNF-5837
CHF 0.00
In stock
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| Product Details | |
|---|---|
| Synonyms | GNF5837 |
| Product Type | Chemical |
| Properties | |
| Formula | C28H21F4N5O2 |
| MW | 535.5 |
| CAS | 1033769-28-6 |
| Purity Chemicals | ≥95% |
| Appearance | Solid. |
| Solubility | Soluble in DMSO. |
| Declaration | Manufactured by SynKinase. |
| Other Product Data |
Target: TRK | Kinase Group: RTK | Substrate: Serine-Threonine Click here for Original Manufacturer Product Datasheet Our product description may differ slightly from the original manufacturers product datasheet. |
| InChi Key | YYDUWLSETXNJJT-MTJSOVHGSA-N |
| Shipping and Handling | |
| Shipping | AMBIENT |
| Short Term Storage | +4°C |
| Long Term Storage | -20°C |
| Use/Stability | Stable for at least 2 years after receipt when stored at -20°C. |
| Documents | |
| MSDS |
 Download PDF |
| Product Specification Sheet | |
| Datasheet |
Download PDF |
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.).
Product 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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