Momelotinib
- CAS No.
- 1056634-68-4
- Chemical Name:
- Momelotinib
- Synonyms
- Orange solid;Momelotinib (CYT387);momelotinib(JAK inhibitor)ORPHAN DRUG;CS-177;LM-1149;CYT 387;GS-0387;CYT 11387;MoMelotinib;CYT387, >=98%
- CBNumber:
- CB22514570
- Molecular Formula:
- C23H22N6O2
- Molecular Weight:
- 414.46
- MDL Number:
- MFCD16038899
- MOL File:
- 1056634-68-4.mol
- MSDS File:
- SDS
| Density | 1.292 |
|---|---|
| storage temp. | Store at -20°C |
| solubility | insoluble in EtOH; insoluble in H2O; ≥20.7 mg/mL in DMSO |
| pka | 10.94±0.46(Predicted) |
| form | Orange powder. |
| CAS DataBase Reference | 1056634-68-4 |
| FDA UNII | 6O01GMS00P |
| NCI Drug Dictionary | momelotinib |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|||||||||
|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302 | |||||||||
| Precautionary statements | P264-P270-P301+P312-P330-P501 | |||||||||
| NFPA 704 |
|
Momelotinib price More Price(31)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 16246 | CYT387 ≥98% | 1056634-68-4 | 1mg | $81 | 2024-03-01 | Buy |
| Cayman Chemical | 16246 | CYT387 ≥98% | 1056634-68-4 | 5mg | $120 | 2024-03-01 | Buy |
| Cayman Chemical | 16246 | CYT387 ≥98% | 1056634-68-4 | 10mg | $184 | 2024-03-01 | Buy |
| Cayman Chemical | 16246 | CYT387 ≥98% | 1056634-68-4 | 50mg | $515 | 2024-03-01 | Buy |
| TRC | C991800 | CYT387 | 1056634-68-4 | 50mg | $415 | 2021-12-16 | Buy |
Momelotinib Chemical Properties,Uses,Production
Description
Momelotinib (CYT387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Phase 3.
In vitro
CYT387 inhibits the proliferation of parental Ba/F3 cells (Ba/F3-wt) stimulated by IL-3 with IC50 of 1400 nM. Furthermore, CYT387 also causes the inhibition of cell proliferation in cell lines constitutively activated by JAK2 or MPL signaling, including Ba/F3-MPLW515L cells, CHRF-288-11 cells and Ba/F3-TEL-JAK2 cells with IC50 of 200 nM, 1 nM and 700 nM, respectively. In addition, CYT387 has been shown to inhibit erythroid colony growth in vitro from JAK2V617F-positive PV patients with similar potency with IC50 of 2μ-4 μM. A recent study shows that CYT387 inhibits PI3K/AKT and Ras/MAPK signaling induced by IL-6 and IGF-1. Moreover, CYT387 induces apoptosis as a single agent and synergizes with the conventional anti-MM therapies bortezomib and melphalan in primary multiple myeloma (MM) cells.
In vivo
In a murine MPN model, CYT387 normalizes white cell counts, hematocrit, spleen size, and restores physiologic levels of inflammatory cytokines.
Uses
CYT387 inhibits Janus kinase 1 (JAK1) and Janus kinase (JAK2). These kinases are part of the JAK-STAT pathway and dysregulated functions are involved with hematology, oncology and inflammatory diseases.
Definition
ChEBI: Momelotinib is a benzamide obtained by formal condensation of the carboxy group of 4-{2-[4-(morpholin-4-yl)anilino]pyrimidin-4-yl}benzoic acid with the primary amino group of aminoacetonitrile. It is an ATP-competitive JAK1/JAK2 inhibitor with IC50 of 11 nM and 18 nM, respectively. Used for the treatment of patients with intermediate- or high-risk myelofibrosis. It has a role as an EC 2.7.10.2 (non-specific protein-tyrosine kinase) inhibitor, an antineoplastic agent, an anti-anaemic agent and an apoptosis inducer. It is an aminopyrimidine, a member of morpholines, a secondary amino compound, a tertiary amino compound, a member of benzamides and a nitrile.
Biological Activity
cyt387, an aminopyrimidine derivative discovered by high-throughput enzyme and cell-based screening along with the optimization using structure-guided medicinal chemistry, is a potent and selective inhibitor of janus kinase 1 (jak1), janus kinase 2 (jak2) and tyrosine kinase 2 (tyk2) with values of 50% inhibition concentration ic50 of 11 nm, 18 nm, 155 nm and 17 nm respectively. recent studies have revealed that cyt387, at low nanomolar concentrations ranging between 500 and 1500 nm, is able to inhibit jak2 signaling pathway, suppress proliferation and induce apoptosis in jak2-dependent hematopoietic cell lines with non-hematopoietic cell lines intact.tyner jw, bumm tg, deininger j, wood l, aichberger kj, loriaux mm, druker bj, burns cj, fantino e, deininger mw. cyt387, a novel jak2 inhibitor, induces hematologic responses and normalizes inflammatory cytokines in murine myeloproliferative neoplasms. blood. 2010;115(25):5232-5240.
target
JAK1
Momelotinib Preparation Products And Raw materials
Raw materials
1of3
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32480 | 60 |
| career henan chemical co | +86-0371-86658258 | sales@coreychem.com | China | 29914 | 58 |
| Biochempartner | 0086-13720134139 | candy@biochempartner.com | CHINA | 967 | 58 |
| Hubei Jusheng Technology Co.,Ltd. | 18871490254 | linda@hubeijusheng.com | CHINA | 28180 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| Chongqing Chemdad Co., Ltd | +86-023-61398051 +8613650506873 | sales@chemdad.com | China | 39916 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49390 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 29220 | 58 |
View Lastest Price from Momelotinib manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2022-09-23 | Momelotinib
1056634-68-4
|
US $0.00-0.00 / KG | 1KG | 98% | 1ton | Henan Aochuang Chemical Co.,Ltd. | |
 |
2021-07-02 | Momelotinib
1056634-68-4
|
US $15.00-10.00 / KG | 1KG | 99%+ HPLC | Monthly supply of 1 ton | Zhuozhou Wenxi import and Export Co., Ltd | |
 |
2019-07-06 | Momelotinib
1056634-68-4
|
US $2.00 / kg | 1kg | 99% | 100kg | Career Henan Chemical Co |
-
- Momelotinib
1056634-68-4
- US $0.00-0.00 / KG
- 98%
- Henan Aochuang Chemical Co.,Ltd.
-
- Momelotinib
1056634-68-4
- US $15.00-10.00 / KG
- 99%+ HPLC
- Zhuozhou Wenxi import and Export Co., Ltd
-
- Momelotinib
1056634-68-4
- US $2.00 / kg
- 99%
- Career Henan Chemical Co