XL019

SIGMA/SML2393 - ≥98% (HPLC)

Synonym: (2S)-N-[4-[2-[[4-(4-Morpholinyl)phenyl]amino]-4-pyrimidinyl]phenyl]-2-pyrrolidinecarboxamide; (S)-N-(4-(2-(4-Morpholinophenylamino)pyrimidin-4-yl)phenyl)pyrrolidine-2-carboxamide; N-(4-{2-[(4-Morpholin-4-ylphenyl)amino]pyrimidin-4-yl}phenyl)-L-prolinamide

CAS Number: 945755-56-6
Empirical Formula (Hill Notation): C₂₅H₂₈N₆O₂
Molecular Weight: 444.53
MDL Number: MFCD24386874
Linear Formula: C₂₅H₂₈N₆O₂
Product Type: Chemical

Catalog Number	PKG Qty.	Price


45-SML2393-5MG	5 mg	$89.00 1/EA	Add To Favorites
45-SML2393-25MG	25 mg	$359.00 1/EA	Add To Favorites

Properties
Descriptions
Safety Info.
Basic Data

assay	≥98% (HPLC)
color	white to beige
form	powder
SMILES string	O=C(NC1=CC=C(C=C1)C2=NC(NC3=CC=C(C=C3)N4CCOCC4)=NC=C2)[C@H]5NCCC5
solubility	DMSO: 2 mg/mL
storage temp.	2-8°C

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).

Symbol	GHS08
Signal word	Danger
Hazard statements	H372
Precautionary statements	P260 - P264 - P270 - P314 - P501
WGK Germany	WGK 3
Flash Point(F)	Not applicable
Flash Point(C)	Not applicable

Purity	≥98% (HPLC)
Storage Temp.	2-8°C
UNSPSC	12352200

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