XL019

XL019

Biochem/physiol Actions

XL019 is an ATP-binding site-targeting, orally active JAK2 subtype-selective Janus kinase inhibitor (IC50 in nM = 2.2/JAK2 vs. 134.3/JAK1, 214.2/JAK3, 348.3/TYK2) with much reduced or little activity against 116 other kinases (IC50 in nM = 125.4/PDGFRB, 139.7/FLT3, 225.8/c-KIT, 313.8/p70S6K, 370/MLK1, 375.4/IKKbeta, 483.6/KDR, 546.7/PDGFRA, 554.5/FLT4, 910.5/FLT; IC50 >1 µM toward remaining 106 kinases), CYP (1A2, 2C9, 2D6, 3A4 IC50 ≥20 µM), hERG (IC50 = 16 µM), and P-glycoprotein (IC50 >20 µM). XL019 effectively inhibits cellular STAT1/STAT3 phosphorylation both in HEL92.1.7 cultures (IC50 in nM = 386.4/pStat1 and 695/pStat3) and in HEL92.1.7 xenograft-derived tumor in mice in vivo (oral ED50 in mg/kg = 42/pStat1 and 210/pStat3) with significant HEL92.1.7 tumor suppression efficacy in mice (by 60% and 70% on day 14, respectively, with 200 and 300 mg/kg bid p.o. dosage).

No detailed specifications are available for this product.

There are no downloads for this product.

Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3576251 XL019 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL
£405.32 (exc VAT) per 25MG
-
+
3576252 XL019 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL
£100.43 (exc VAT) per 5MG
-
+