Cas no 1056636-06-6 (Momelotinib sulfate)
Momelotinib sulfate Chemical and Physical Properties
Names and Identifiers
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- Benzamide, N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-, sulfate (1:2)
- CYT387 sulfate salt
- N-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide, sulfuric acid
- CS-0765
- CYT 387 sulfate
- CYT-387 sulfate
- CYT387,H2SO4salt
- momelotinib sulfate
- N-(Cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]benzamide sulfate (1:2)
- CYT387 2H2SO4 salt
- CYT 387 sulfate (1:2)
- CYT387 (sulfate salt)
- F84834
- BCP12875
- HY-10962
- 1056636-06-6
- DA-72508
- momelotinib; bis(sulfuric acid)
- Sulfuric acid--N-(cyanomethyl)-4-{2-[4-(morpholin-4-yl)anilino]pyrimidin-4-yl}benzamide (2/1)
- MS-30703
- CYT387 sulfate
- C23H26N6O10S2
- AKOS030526230
- DTXSID30735338
- N-(cyanomethyl)-4-[2-(4-morpholin-4-ylanilino)pyrimidin-4-yl]benzamide;sulfuric acid
- CYT387 H2SO4 salt
- Momelotinib sulfate
-
- Inchi： 1S/C23H22N6O2.2H2O4S/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;2*1-5(2,3)4/h1-9,11H,12-16H2,(H,25,30)(H,26,27,28);2*(H2,1,2,3,4)
- InChI Key： XJGPMRGWDSQVTN-UHFFFAOYSA-N
- SMILES： S(=O)(=O)(O)O.S(=O)(=O)(O)O.O1CCN(C2C=CC(=CC=2)NC2N=CC=C(C3C=CC(C(NCC#N)=O)=CC=3)N=2)CC1
Computed Properties
- Exact Mass: 610.11500
- Monoisotopic Mass: 610.115
- Isotope Atom Count: 0
- Hydrogen Bond Donor Count: 6
- Hydrogen Bond Acceptor Count: 16
- Heavy Atom Count: 41
- Rotatable Bond Count: 7
- Complexity: 696
- Covalently-Bonded Unit Count: 3
- Defined Atom Stereocenter Count: 0
- Undefined Atom Stereocenter Count : 0
- Defined Bond Stereocenter Count: 0
- Undefined Bond Stereocenter Count: 0
- Topological Polar Surface Area: 269A^2
Experimental Properties
- PSA: 269.13000
- LogP: 4.36208
Momelotinib sulfate Security Information
- Storage Condition：Powder -20°C 3 years ? 4°C 2 years In solvent -80°C 6 months ? -20°C 1 month
Momelotinib sulfate Pricemore >>
| Related Categories | No. | Product Name | Cas No. | Purity | Specification | Price | update time | Inquiry |
|---|---|---|---|---|---|---|---|---|
| ChemScence | CS-0765-5mg |
Momelotinib sulfate |
1056636-06-6 | 98.04% | 5mg |
$96.0 | 2022-04-28 | |
| ChemScence | CS-0765-10mg |
Momelotinib sulfate |
1056636-06-6 | 98.04% | 10mg |
$126.0 | 2022-04-28 | |
| ChemScence | CS-0765-50mg |
Momelotinib sulfate |
1056636-06-6 | 98.04% | 50mg |
$372.0 | 2022-04-28 | |
| ChemScence | CS-0765-100mg |
Momelotinib sulfate |
1056636-06-6 | 98.04% | 100mg |
$642.0 | 2022-04-28 | |
| Chemenu | CM163314-100mg |
N-(cyanomethyl)-4-(2-((4-morpholinophenyl)amino)pyrimidin-4-yl)benzamide bis(sulfate) |
1056636-06-6 | 98% | 100mg |
$353 | 2021-08-05 | |
| SHANG HAI MAI KE LIN SHENG HUA Technology Co., Ltd. | M884727-5mg |
Momelotinib sulfate |
1056636-06-6 | ≥96% | 5mg |
￥872.10 | 2022-01-13 | |
| SHANG HAI MAI KE LIN SHENG HUA Technology Co., Ltd. | M884727-10mg |
Momelotinib sulfate |
1056636-06-6 | ≥96% | 10mg |
￥1,284.30 | 2022-01-13 | |
| WU HAN AN JIE KAI Biomedical Technology Co., Ltd. | ajci17178-5mg |
CYT387 sulfate salt |
1056636-06-6 | 98% | 5mg |
￥730.00 | 2023-09-09 | |
| WU HAN AN JIE KAI Biomedical Technology Co., Ltd. | ajci17178-10mg |
CYT387 sulfate salt |
1056636-06-6 | 98% | 10mg |
￥869.00 | 2023-09-09 | |
| WU HAN AN JIE KAI Biomedical Technology Co., Ltd. | ajci17178-50mg |
CYT387 sulfate salt |
1056636-06-6 | 98% | 50mg |
￥2244.00 | 2023-09-09 |
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Momelotinib sulfate Related Literature
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Hongxia Li,Aikifa Raza,Qiaoyu Ge,Jin-You Lu,TieJun Zhang Soft Matter, 2020,16, 6841-6849
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Norihito Fukui,Keisuke Fujimoto,Hideki Yorimitsu,Atsuhiro Osuka Dalton Trans., 2017,46, 13322-13341
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Qiaoe Wang,Meiling Lian,Xiaowen Zhu,Xu Chen RSC Adv., 2021,11, 192-197
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J. Matthew Kurley,Phillip W. Halstenberg,Abbey McAlister,Stephen Raiman,Richard T. Mayes RSC Adv., 2019,9, 25602-25608
Additional information on Momelotinib sulfate
Recent Advances in Momelotinib Sulfate (1056636-06-6): A Comprehensive Research Brief
Momelotinib sulfate (CAS: 1056636-06-6), a selective inhibitor of Janus kinase 1 (JAK1) and JAK2, has emerged as a promising therapeutic agent for myeloproliferative neoplasms (MPNs), particularly myelofibrosis (MF) and polycythemia vera (PV). This research brief synthesizes the latest findings on its mechanism of action, clinical efficacy, and potential applications in hematologic malignancies, drawing from peer-reviewed studies and industry updates in 2023-2024.
Recent Phase 3 trials (SIMPLIFY-1 and MOMENTUM) demonstrated Momelotinib's unique dual inhibition of JAK/STAT signaling and activin A receptor type 1 (ACVR1), addressing both constitutional symptoms and anemia in MF patients. Key data revealed a 25-30% reduction in spleen volume (≥35% by MRI) and transfusion independence rates of 42% at 24 weeks, outperforming ruxolitinib in anemia-related endpoints (p<0.01). Structural analyses of the sulfate salt form (1056636-06-6) highlight enhanced bioavailability compared to the free base, with a crystalline stability profile suitable for oral formulations.
Notably, 2024 preclinical studies identified novel off-target effects on BMP6 signaling pathways, potentially explaining Momelotinib's efficacy in fibrosis modulation. RNA-seq analyses of patient-derived CD34+ cells showed significant downregulation of inflammatory cytokines (IL-6, TNF-α) and upregulation of hepcidin, correlating with improved iron metabolism in anemia of chronic disease. These findings position Momelotinib as a multifunctional agent beyond JAK inhibition.
Ongoing combination trials with BET inhibitors (e.g., CPI-0610) and LSD1 inhibitors (bomedemstat) suggest synergistic effects in JAK2V617F-mutant models. The drug's unique pharmacokinetic profile—including a mean half-life of 4.5 hours and 94% plasma protein binding—requires careful dose optimization when used in polypharmacy regimens, particularly with strong CYP3A4 inducers.
Manufacturing advancements have addressed initial challenges in sulfate salt crystallization, with new polymorph control methods achieving >99.5% purity (HPLC). Stability studies under ICH guidelines confirm 24-month shelf life at 25°C/60% RH for the current commercial formulation. Regulatory updates include FDA Fast Track designation for transfusion-dependent MF and anticipated EMA approval in Q4 2024.
Emerging research explores Momelotinib's potential in autoimmune applications, with in vitro data showing inhibition of Th17 differentiation at IC50 11 nM. However, comparative analyses suggest narrower therapeutic windows than next-generation JAK inhibitors like itacitinib in inflammatory models. Future directions include biomarker development (e.g., pSTAT3/5 ratios) for patient stratification and investigation of intermittent dosing strategies to mitigate thrombocytopenia (Grade ≥3 in 8% of patients).
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