| Size | Price | Stock | Qty |
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| 5mg |
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Momelotinib sulfate (CYT387) is a novel and potent inhibitor of JAK1/JAK2 with with potential antitumor and anti-inflammatory activity. It inhibits JAK1/2 with IC50 of 11 nM/18 nM, 10-fold selectivity versus JAK3 (IC50=155 nM). Momelotinib (Ojjaara) was approved in 2023 by FDA for treating Myelofibrosis in adults with anaemia.
| ln Vitro |
Momelotinib sulfate, also known as CYT387 sulfate salt, suppresses the growth of Ba/F3-JAK2V617F and human erythroleukemia (HEL) cells (IC50=1.5 μM) or Ba/F3-MPLW515L cells (IC50=200 nM). However, it exhibits significantly less activity against K562 cells that harbor BCR-ABL (IC50=58 μM) and MV4-11 cells that harbor FLT3 mutation (IC50=3 μM). With an IC50 value of 1.4 μM, the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated with IL-3 is suppressed, in keeping with the known function of IL-3-dependent signaling in the parental cell line[1].
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| ln Vivo |
Over the course of eight weeks, momelotinib sulfate (CYT387 sulfate salt), at twice the dose employed in the illness model (50 and 100 mg/kg), has little to no effect on peripheral blood counts. With a half-life of roughly two hours, the median plasma peak concentrations are 7.1 μM for the lower dose and 32.1 μM for the higher dose. Twelve-hour trough values for the 25 mg/kg and 50 mg/kg doses, respectively, are 10nM and 900nM. The cohort's average white blood cell counts and hematocrit values at day 34 post-transplantation were more than one standard deviation above the usual range for Balb/c mice. Six mice are now sacrificed and put through an autopsy. Treatment is started twice daily by oral gavage (12 mice per treatment group) with 25 mg/kg Momelotinib sulfate (CYT387 sulfate salt), 50 mg/kg Momelotinib sulfate (CYT387 sulfate salt), or vehicle for the remaining animals. Within 6 days of treatment beginning, both dose cohorts show a sharp reduction in white cell counts, and after 20 days, there is a noticeable decline in hematocrit[2]. Momelotinib sulfate (CYT387 sulfate salt) has an apparent half life of 2.4 hours, a quantitative absolute oral bioavailability, and high plasma concentrations (Cmax= 40.4 μM; Tmax= 4 h) following oral administration. The low blood clearance of momelotinib sulfate (CYT387 sulfate salt) (6.3 mL/min/kg) and consequently poor susceptibility to hepatic first pass metabolism are probably contributing factors to the drug's high oral bioavailability[3].
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| References |
[1]. Pardanani A, et al. CYT387, a selective JAK1/JAK2 inhibitor: in vitro assessment of kinase selectivity and preclinical studies using cell lines and primary cells from polycythemia vera patients. Leukemia, 2009, 23(8), 1441-1445.
[2]. Tyner JW, et al. CYT387, a novel JAK2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. Blood, 2010, 115(25), 5232-5240. [3]. Burns CJ, et al. Phenylaminopyrimidines as inhibitors of Janus kinases (JAKs). Bioorg Med Chem Lett. 2009 Oct 15;19(20):5887-92 |
| Molecular Formula |
C23H22N6O2.2[H2O4S]
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|---|---|
| Molecular Weight |
610.61674
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| CAS # |
1056636-06-6
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| Related CAS # |
Momelotinib;1056634-68-4;Momelotinib Mesylate;1056636-07-7
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| SMILES |
O=C(NCC#N)C(C=C1)=CC=C1C2=NC(NC(C=C3)=CC=C3N4CCOCC4)=NC=C2.O=S(O)(O)=O.O=S(O)(O)=O
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| Synonyms |
Ojjaara
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
DMSO : ~220 mg/mL (~360.29 mM)
H2O : ~100 mg/mL (~163.77 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5.5 mg/mL (9.01 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 55.0 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. Solubility in Formulation 2: ≥ 5.5 mg/mL (9.01 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 55.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5.5 mg/mL (9.01 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (163.77 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6377 mL | 8.1884 mL | 16.3768 mL | |
| 5 mM | 0.3275 mL | 1.6377 mL | 3.2754 mL | |
| 10 mM | 0.1638 mL | 0.8188 mL | 1.6377 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.
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