Products List
Products
Home > Product List > API >

XL019 945755-56-6

1.Inquiries will be replied within 24 hours
2.We could supply various packages as you required
3.To protect the profit of our agents, price will not show on website, please send inquiries to get the price.
4.Fast delivery, goods arrive your office within 3 to 5 days
5.Please click "Inquiry" or "Email" below to get the price
　
Synonyms ：
Appearance ：
Chemical Formula ：
C25H28N6O2
Solubility ：
Molecular Weight ：
444.53
Storage and Stability ：
in stock
CAS No. ：
945755-56-6
Purity ：
98%+
Introduction
XL019 is a highly selective JAK2 inhibitor, binds to the active site of JAK2 displaying >50-fold selectivity against JAK1 and TYK2. XL019 reveals a desirable CYP (1A2, 2C9, 2D6, 3A4 ≥20 μM), hERG (16 μM), and P-glycoprotein inhibition (>20 μM) profile. XL019 inhibits the activation of JAK2 as well as the mutated form JAK2V617F, which may result in the inhibition of the JAK-STAT signaling pathway and may induce apoptosis. XL019 showed more than 10-fold selective inhibition (IC50 = 64 nM) of STAT5 phosphorylation following EPO stimulation of erythroid cells compared with other cell systems.

XL019 significantly inhibits downstream markers pSTAT1 and pSTAT3 after administration 30, 100, and 300 mg/kg resulting in an ED50 of 42 mg/kg (pSTAT1) and 210 mg/kg (pSTAT3). XL019 has a superior pharmacodynamic profile and exhibits good oral absorption, and modest clearance and half life across species. XL019 inhibits of HEL.92.1.7 xenograft tumors growth in mice. It demonstrates 60% and 70% inhibition when dosed orally at 200 mg/kg and 300 mg/kg respectively twice a day for 14 days. Dosing at 300 mg/kg bid provided an 11.3-fold increase in apoptosis relative to vehicle control. 

Products for scientific research use only

Thank you for your company product support!

CAS No. ：

Product Name ：

Number ：

Your name：
*

Phone：

Email：
*

The company or laboratory name：
*