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Purity: ≥98%
XL019 (XL-019) is a novel, potent and selective and orally bioavailable inhibitor of Janus kinase-JAK2 with potential antitumor activity. It inhibits JAK2 with an IC50 of 2.2 nM, and exhibits >50-fold selectivity for JAK2 over JAK1, JAK3 and TYK2. It shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. 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. The JAK2 mutated form JAK2V617F has a valine-to-phenylalanine modification at position 617 and plays a key role in tumor cell proliferation and survival.
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| ln Vivo |
XL019 (po; twice daily for 14 days; 100–300 mg/kg) suppresses the formation of HEL.92.1.7 xenograft tumors[1]. The Cmax, t1/2, and Vd for XL019 (10 mg/kg) dosing were 5.24 μM, 1.94 hours, and 5.319 L/kg, respectively[1].
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| Animal Protocol |
Animal/Disease Models: Female nude mice (HEL.92.1.7 xenograft tumors)[1]
Doses: 100, 200, 300 mg/kg Route of Administration: po; twice (two times) daily for 14 days Experimental Results: Inhibition of HEL.92.1.7 xenograft tumor growth. Animal/Disease Models: Mouse[1] Doses: 10 mg/kg Route of Administration: po(pharmacokinetic/PK Analysis) Experimental Results: The Cmax, t1/2 and Vd were 5.24 μM, 1.94 hrs (hours), and 5.319 L/kg, respectively. |
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| References |
[1]. Forsyth T, et al. SAR and in vivo evaluation of 4-aryl-2-aminoalkylpyrimidines as potent and selective Janus kinase 2 (JAK2) inhibitors. Bioorg Med Chem Lett. 2012 Dec 15;22(24):7653-8.
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| Molecular Formula |
C25H28N6O2
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| Molecular Weight |
444.53
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| CAS # |
945755-56-6
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| Related CAS # |
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| SMILES |
O1C([H])([H])C([H])([H])N(C2C([H])=C([H])C(=C([H])C=2[H])N([H])C2=NC([H])=C([H])C(C3C([H])=C([H])C(=C([H])C=3[H])N([H])C([C@]3([H])C([H])([H])C([H])([H])C([H])([H])N3[H])=O)=N2)C([H])([H])C1([H])[H]
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| InChi Key |
ISOCDPQFIXDIMS-QHCPKHFHSA-N
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| InChi Code |
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
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| Chemical Name |
(S)-N-(4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)phenyl)pyrrolidine-2-carboxamide
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00595829 | Terminated | Drug: XL019 | Polycythemia Vera | Exelixis | December 2007 | Phase 1 |
| NCT00522574 | Terminated | Drug: XL019 | Myeloproliferative Disorders Myelofibrosis |
Exelixis | August 2007 | Phase 1 |
Bioorg Med Chem Lett.2012Dec 15;22(24):7653-8. |
Bioorg Med Chem Lett.2012Dec 15;22(24):7653-8. |
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