| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Momelotinib (formerly CYT-387; CYT-11387; LM-1149; Ojjaara), an aminopyrimidine analog, is a novel, potent and ATP-competitive inhibitor of Janus kinases (JAK1/2) with potential antitumor and anti-inflammatory activity. It inhibits JAK1/2 with IC50s of 11 nM/18 nM, and shows ~10-fold selectivity for JAK1/2 over JAK3. CYT 387 is currently undergoing Phase I/II clinical trials for treating myelofibrosis. Momelotinib shows potent in vitro antiproliferative activity and high in vivo antitumor efficacy. It was discovered by high-throughput enzyme and cell-based screening along with the optimization using structure-guided medicinal chemistry. Momelotinib (Ojjaara) was approved in 2023 by FDA for treating Myelofibrosis in adults with anaemia.
| ln Vitro |
Momelotinib (CYT387) has an IC50 of 1400 nM, which suppresses the proliferation of parental Ba/F3 cells (Ba/F3-wt) triggered by IL-3. Furthermore, Momelotinib (CYT387), with an IC50 of 200, reduces the proliferation of cell lines activated by JAK2 or MPL signaling, such as Ba/F3-MPLW515L cells, CHRF-288-11 cells, and Ba/F3-TEL-JAK2 cells. 700 nM, 1 nM, and nM. Furthermore, it has been demonstrated that momelotinib (CYT387), with an IC50 of 2 μM–4 μM, also potently inhibits the formation of erythrocyte colonies in individuals with JAK2V617F-positive PV in vitro [1]. IGF-1 and IL-6-induced Ras/MAPK and PI3K/AKT activation are inhibited by momelotinib (CYT387). Additionally, in primary multiple myeloma (MM) cells, momelotinib (CYT387) promotes apoptosis as a single agent and synergizes with conventional anti-MM medications PS-341 and L-PAM [2].
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| ln Vivo |
Momelotinib (CYT387) corrected hematocrit, spleen size, white blood cell count, and physiological levels of inflammatory cytokines in a mouse model of MPN [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]. Monaghan KA, et al. The novel JAK inhibitor CYT387 suppresses multiple signalling pathways, prevents proliferation and induces apoptosis in phenotypically diverse myeloma cells. Leukemia, 2011, 25(12), 1891-1899. [3]. 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. [4]. Kitajima S, et al.Overcoming Resistance to Dual Innate Immune and MEK Inhibition Downstream of KRAS.Cancer Cell. 2018 Sep 10;34(3):439-452.e6 |
| Molecular Formula |
C23H22N6O2
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|---|---|
| Molecular Weight |
414.46
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| CAS # |
1056634-68-4
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| Related CAS # |
Momelotinib sulfate;1056636-06-6;Momelotinib Mesylate;1056636-07-7
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| SMILES |
O=C(NCC#N)C1=CC=C(C2=NC(NC3=CC=C(N4CCOCC4)C=C3)=NC=C2)C=C1
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| InChi Key |
ZVHNDZWQTBEVRY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H22N6O2/c24-10-12-25-22(30)18-3-1-17(2-4-18)21-9-11-26-23(28-21)27-19-5-7-20(8-6-19)29-13-15-31-16-14-29/h1-9,11H,12-16H2,(H,25,30)(H,26,27,28)
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| Chemical Name |
N-(cyanomethyl)-4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)benzamide.
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| Synonyms |
LM-1149 , CYT-11387; LM 1149 , CYT 11387; LM1149 , CYT11387; CYT-387; Momelotinib; Momelotinib free base; CYT387; CYT 387; 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.03 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 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. Solubility in Formulation 2: 30% PEG400+0.5% Tween80+5% propylene glycol: 30 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4128 mL | 12.0639 mL | 24.1278 mL | |
| 5 mM | 0.4826 mL | 2.4128 mL | 4.8256 mL | |
| 10 mM | 0.2413 mL | 1.2064 mL | 2.4128 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 |
| NCT02244489 | Terminated | Drug: Momelotinib (MMB) Drug: Capecitabine |
Relapsed/Refractory Metastatic Pancreatic Ductal Adenocarcinoma |
Sierra Oncology LLC - a GSK company |
November 5, 2014 | Phase 1 |
| NCT02206763 | Terminated | Drug: Momelotinib (MMB) Drug: Erlotinib |
EGFR Mutated EGFR TKI Naive Metastatic NSCLC |
Sierra Oncology LLC - a GSK company |
October 16, 2014 | Phase 1 |
| NCT01998828 | Terminated | Drug: Larotrectinib Sulfate Procedure: Bone Scan |
Drug: Momelotinib | Polycythemia Vera Essential Thrombocythemia |
February 19, 2014 | Phase 2 |
| NCT02258607 | Terminated | Drug: Momelotinib (MMB) Drug: Trametinib |
Relapsed Metastatic KRAS-Mutated Non-Small Cell Lung Cancer |
Sierra Oncology LLC - a GSK company |
March 11, 2015 | Phase 1 |
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