XL019

JAK2 inhibitor,potent and selective CAS# 945755-56-6

XL019

Catalog No. BCC2057----Order now to get a substantial discount!

Product Name & Size Price Stock
XL019:5mg $90.00 In stock
XL019:10mg $153.00 In stock
XL019:25mg $360.00 In stock
XL019:50mg $630.00 In stock
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Quality Control of XL019

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Chemical structure

XL019

3D structure

Chemical Properties of XL019

Cas No. 945755-56-6 SDF Download SDF
PubChem ID 57990869 Appearance Powder
Formula C25H28N6O2 M.Wt 444.53
Type of Compound N/A Storage Desiccate at -20°C
Solubility DMSO : 25 mg/mL (56.24 mM; Need ultrasonic)
Chemical Name (2S)-N-[4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]phenyl]pyrrolidine-2-carboxamide
SMILES C1CC(NC1)C(=O)NC2=CC=C(C=C2)C3=NC(=NC=C3)NC4=CC=C(C=C4)N5CCOCC5
Standard InChIKey ISOCDPQFIXDIMS-QHCPKHFHSA-N
Standard InChI InChI=1S/C25H28N6O2/c32-24(23-2-1-12-26-23)28-19-5-3-18(4-6-19)22-11-13-27-25(30-22)29-20-7-9-21(10-8-20)31-14-16-33-17-15-31/h3-11,13,23,26H,1-2,12,14-17H2,(H,28,32)(H,27,29,30)/t23-/m0/s1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of XL019

DescriptionXL019 is a potent and selective inhibitor of JAK2 with IC50 value of 2.2 nM.
TargetsJAK2    
IC502.2 nM     

XL019 Dilution Calculator

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XL019 Molarity Calculator

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Preparing Stock Solutions of XL019

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2496 mL 11.2478 mL 22.4957 mL 44.9913 mL 56.2392 mL
5 mM 0.4499 mL 2.2496 mL 4.4991 mL 8.9983 mL 11.2478 mL
10 mM 0.225 mL 1.1248 mL 2.2496 mL 4.4991 mL 5.6239 mL
50 mM 0.045 mL 0.225 mL 0.4499 mL 0.8998 mL 1.1248 mL
100 mM 0.0225 mL 0.1125 mL 0.225 mL 0.4499 mL 0.5624 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on XL019

XL019 is a potent and selective inhibitor of JAK2 with IC50 value of 2.2 nM.
JAK kinases were first identified in 1989 and characterized by the presence of two tyrosine kinase domains. There are four members in the JAK family, which are JAK1, JAK2, JAK3 and TYK2. JAK2 played an important role in the pathways that control erythroid, myeloid and megakaryocytic development. JAK2 mediates signaling through erythropoietin receptor, thrombopoietin receptor and cytokine receptor that harbor the common β-chain (e.g. IL3 receptor) and IFN-γ receptors [38]. JAK2 inhibitors are a novel class of agents with promising results for treating patients with polycythemia vera (PV), essential thrombocythemia (ET) and myelofibrosis (MF) [1]. XL019 was selected as a clinical candidate and advanced into human clinical trials where it was evaluated in patients with PMF, post-PV, or post-ET MF [2].
XL019 shows good biochemical and cellular potency against JAK2 with good selectivity, against a panel of over 100 serine/threonine and tyrosine kinases, including other members of the JAK family [2]. Analogue XL019 was evaluated against a select panel of 118 kinases. Targets for which XL019 exhibited IC50 <1000 nM are displayed. XL019 is a highly selective JAK2 inhibitor displaying >50-fold selectivity against all kinases tested including JAK1 and TYK2. XL019 was a desirable CYP, hERG (16 μM), and P-glycoprotein inhibition (>20 μM).
XL019 had a superior pharmacodynamic profile and thus was evaluated in an efficacy experiment measuring growth inhibition of HEL.92.1.7 xenograft tumors in mice. Derivative XL019 demonstrated 60% and 70% inhibition when dosed orally at 200 mg/kg and 300 mg/kg respectively twice a day for 14 days. Thirty patients received XL019 for a median of 91 days. All of them have discontinued XL019 therapy. Toxicity: N/A Clinical trial: A Safety Study of XL-019 in Adults With Myelofibrosis [2].
References:
[1]. Fabio P.S. Santos, Srdan Verstovsek. JAK2 inhibitors: What's the true therapeutic potential?. Blood Reviews, 2011, 25: 53-63.
[2]. Srdan Verstovsek, Constantine S. Tam, Martha Wadleigh, et al. Phase I evaluation of XL019, an oral, potent, and selective JAK2 inhibitor. Leukemia Research, 2014, 38: 316-322.

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References on XL019

Phase I evaluation of XL019, an oral, potent, and selective JAK2 inhibitor.[Pubmed:24374145]

Leuk Res. 2014 Mar;38(3):316-22.

This phase I study evaluated selective JAK2 inhibitor XL019 in 30 patients with myelofibrosis. The initial dose cohorts were 100, 200, and 300 mg orally on days 1-21 of a 28-day cycle. Central and/or peripheral neurotoxicity developed in all patients. Subsequently, patients were treated on lower doses; neurotoxicity was again observed, leading to study termination. Peripheral neuropathy resolved in 50%, and central neurotoxicity in all patients within months after therapy cessation. Myelosuppression was minimal. The terminal half-life of XL019 was approximately 21 h, with steady state reached by Day 8. International Working Group defined responses were seen in three (10%) patients.

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.

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