Momelotinib

Description In vitro In vivo

Product Name: 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
Formula Weight: 414.46
MOL File: 1056634-68-4.mol

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Momelotinib Property

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.
color: Light yellow to yellow
CAS DataBase Reference: 1056634-68-4

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

Precautionary statements

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P330Rinse mouth.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 16246
Product name: CYT387
Purity: ≥98%
Packaging: 1mg
Price: $81
Updated: 2024/03/01

Cayman Chemical

Product number: 16246
Product name: CYT387
Purity: ≥98%
Packaging: 5mg
Price: $120
Updated: 2024/03/01

Cayman Chemical

Product number: 16246
Product name: CYT387
Purity: ≥98%
Packaging: 10mg
Price: $184
Updated: 2024/03/01

Cayman Chemical

Product number: 16246
Product name: CYT387
Purity: ≥98%
Packaging: 50mg
Price: $515
Updated: 2024/03/01

TRC

Product number: C991800
Product name: CYT387
Packaging: 50mg
Price: $415
Updated: 2021/12/16

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Momelotinib Chemical Properties,Usage,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

Preparation Products

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Momelotinib Suppliers

China 186 India 2 United Kingdom 1 United States 21 Global 210

xinguokeji

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Shanghai JiYi Biotechnology Co. Ltd.

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ShangHai Biochempartner Co.,Ltd

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Shanghai Dongyang Biotechnology Co., Ltd.

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Chunchuang (Wuhan) Technology Co., Ltd

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JINAN RUIFENG PHARMACEUTICAL TECHNOLOGY CO.,LTD

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Shanghai Boyle Chemical Co., Ltd.

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Chembest Research Laboratories Limited

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Jinan Trio PharmaTech Co., Ltd.

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Dalian Meilun Biotech Co., Ltd.

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View Lastest Price from Momelotinib manufacturers

Zhuozhou Wenxi import and Export Co., Ltd

Product: Momelotinib 1056634-68-4
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-06-26

Career Henan Chemical Co

Product: Momelotinib 1056634-68-4
Price: US $2.00/kg
Min. Order: 1kg
Purity: 99%
Supply Ability: 100kg
Release date: 2018-12-23

1056634-68-4, MomelotinibRelated Search:

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momelotinib(JAK inhibitor)ORPHAN DRUG

CYT387, >=98%

CYT 11387

CYT 387

N-(Cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]benzamide

LM-1149

CYT 387(CYT 11387)

N-(cyanoMethyl)-4-(2-(4-Morpholin-4-ylphenylaMino)pyriMidin-4-yl)benzaMide

MoMelotinib

Benzamide,N-(cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]-

CYT387;CYT 387; CYT-387

Orange solid

N-(Cyanomethyl)-4-(2-((4-morpholinophenyl)-amino)pyrimidin-4-yl)benzamide

CYT 11387;CYT387 (CYT 387);MOMELOTINIB

Momelotinib (CYT387)

N-(Cyanomethyl)-4-[2-[[4-(4-morpholinyl)phenyl]amino]-4-pyrimidinyl]benzamide CYT 387

CYT387(momelotinib)

GS-0387

CS-177

Momelotinib (CYT387,CYT-387)

CYT 11387;CYT387 (CYT 387)

CYT387 (CYT 387)

Momelotinib USP/EP/BP

Momelotinib (LM1149

N-(Cyanomethyl)-4-[2-[(4-morpholinophenyl)amino]-4-pyrimidinyl]benzamide

Momelotinib (PF-06651600)

Momelotinib free base

1056634-68-4

API

Inhibitor

Anti-cancer

Inhibitors