XL019

SKU: orb1304569

Description

XL019 is a highly selective small molecule inhibitor of JAK2, exhibiting potent activity with an IC50 of 2.2 nM and demonstrating 100-fold selectivity against JAK1. It is a valuable research tool for studying JAK2-dependent signaling in cellular assays and has been utilized in preclinical models of myeloproliferative neoplasms.

Research Area

Cardiovascular Research, Cell Biology, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

−

Key Properties

−

CAS Number	945755-56-6
MW	444.53
Purity	99.19%
Formula	C₂₅H₂₈N₆O₂
SMILES	O=C(Nc1ccc(cc1)-c1ccnc(Nc2ccc(cc2)N2CCOCC2)n1)[C@@H]1CCCN1
Target	Apoptosis,FLT,JAK,PDGFR
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.5 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:13 mg/mL (29.24 mM)

Bioactivity

−

Target IC50	JAK3:214.2 nM\|JAK2:2.2 nM
In Vivo	L019 inhibits the activation of both JAK2 and its mutant form, JAK2V617F, leading to suppression of the JAK-STAT signaling pathway and inducing apoptosis. Compared to other cellular systems, upon EPO stimulation of the erythroid lineage, L019 demonstrates more than a tenfold selective inhibition of STAT5 phosphorylation (IC50 = 64 nM). Read more...
In Vitro	XL019 exhibits superior pharmacokinetic properties, demonstrating efficient oral absorption, moderate clearance rates, and half-life across various species. Administration of XL019 at 30, 100, and 300 mg/kg significantly inhibits the downstream markers pSTAT1 and pSTAT3, with the effective dose (ED50) for pSTAT1 being 42 mg/kg and for pSTAT3, 210 mg/kg. Furthermore, XL019 effectively suppresses the growth of HEL.92.1.7 xenograft tumors in mice, with dosages of 200 mg/kg and 300 mg/kg administered twice daily for 14 days, achieving tumor growth inhibition rates of 60% and 70%, respectively. Read more...

Storage & Handling

−

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

−

FLT3, Inhibitor, oral, inhibit, JAK2, JAK1, JAK, Janus kinase, JAK3, Apoptosis, antitumor,HEL.92.1.7, cells, tumor, PDGFRβ, selective, phosphorylation, XL 019, XL019, XL-019

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID

57990869 ↗

Key Properties

−

No computed properties available.

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols

XL019 (orb1304569)

Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

No reviews yet

Purity:	>98%(HPLC)
CAS Number:	945755-56-6
MW:	444.5
Formula:	C₂₅H₂₈N₆O₂

XL019

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Similar Products

XL019 [orb1223549]

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

Request a Document

Protocol Information

XL019 (orb1304569)

Step 1: Enter information below

Step 2: Enter the in vivo formulation

Available Sizes

Email

UK Office

US Office

CN Office

Distributors