1. Epigenetics
    Stem Cell/Wnt
    JAK/STAT Signaling
    Apoptosis
  2. JAK
    Apoptosis
  3. XL019

XL019 

Cat. No.: HY-13775 Purity: >98.0%
Handling Instructions

XL019 is a potent,orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2.

For research use only. We do not sell to patients.

XL019 Chemical Structure

XL019 Chemical Structure

CAS No. : 945755-56-6

Size Price Stock Quantity
10 mM * 1  mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
50 mg USD 250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 3 publication(s) in Google Scholar

Top Publications Citing Use of Products

View All JAK Isoform Specific Products:

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

XL019 is a potent,orally active, and selective JAK2 inhibitor, with IC50s of 2.2, 134.3, and 214.2 nM for JAK2, JAK1 and JAK3, respectively. XL019 shows 50-fold or greater selectivity for JAK2, versus a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family. XL019 potently inhibits STAT3 and STAT5 phosphorylation in cells harboring either JAK2V617F or wild-type JAK2[1][2].

IC50 & Target[1]

JAK2

2.2 nM (IC50)

JAK3

214.2 nM (IC50)

In Vivo

XL019 (100-300 mg/kg; p.o.; twice daily for 14 days) inhibits HEL.92.1.7 xenograft tumor growth[1].
XL019 (10 mg/kg) treatment shows that the Cmax, t1/2 and Vd were 5.24 μM, 1.94 hours, 5.319 L/kg, respectively[1].

Animal Model: Female nude mice (HEL.92.1.7 xenograft tumors)[1]
Dosage: 100, 200, 300 mg/kg
Administration: p.o.; twice daily for 14 days
Result: Inhibition of HEL.92.1.7 xenograft tumor growth.
Animal Model: Mouse[1]
Dosage: 10 mg/kg
Administration: p.o.(Pharmacokinetic Analysis)
Result: The Cmax, t1/2 and Vd were 5.24 μM, 1.94 hours, and 5.319 L/kg, respectively.
Clinical Trial
Molecular Weight

444.53

Formula

C₂₅H₂₈N₆O₂

CAS No.

945755-56-6

SMILES

O=C([[email protected]]1NCCC1)NC2=CC=C(C3=NC(NC4=CC=C(N5CCOCC5)C=C4)=NC=C3)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (56.24 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2496 mL 11.2478 mL 22.4957 mL
5 mM 0.4499 mL 2.2496 mL 4.4991 mL
10 mM 0.2250 mL 1.1248 mL 2.2496 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: >98.0%

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

XL019XL 019XL-019JAKApoptosisJanus kinaseselectiveoraltumorphosphorylationantitumor,HEL.92.1.7cellsInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
XL019
Cat. No.:
HY-13775
Quantity:
MCE Japan Authorized Agent: