Momelotinib (CYT387) - Moligand™, 10mM in DMSO , Tyrosine-protein kinase JAK2 inhibitor, CAS No.1056634-68-4, Tyrosine-protein kinase JAK2 inhibitor

CAS: 1056634-68-4 Cat. No.: M408149 Peso molecular: 414.47 Número EC: 894-079-6
Disponible para pedir
GRADE & PURITY Moligand™ ? Moligand™ — Aladdin's line of ligands and bioactive small molecules. Use for receptor, pathway, and binding studies needing defined small-molecule tools. 10mM in DMSO
Synonyms
LM-1149 , CYT11387 | N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
 ·  off list, applied to all prices below.
Size
Estado
Price
Qty
1ml
M408149-1ml
1

181,90US$

263,90US$
Guardar 82,00 US$ (31.07%)
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Why this grade

Moligand™, 10mM in DMSO Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.

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Storage & shipping

Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.

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Quality documents

SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.

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Literature proof

Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.

Descripción general

Information

Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor ofJAK1/JAK2withIC50of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) inducesapoptosisandautophagy. 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.
Cell Data

cell lines:

Concentrations:0 to 10 μM

Incubation Time:72 hours

Powder Purity:≥95%

Specifications

Sinónimos
LM-1149 , CYT11387 | N-(cyanomethyl)-4-(2-(4-morpholinophenylamino)pyrimidin-4-yl)benzamide
Especificaciones y pureza
Moligand™, 10mM in DMSO
Mecanismos bioquímicos y fisiológicos
Momelotinib (CYT387, LM-1149 , CYT11387) is an ATP-competitive inhibitor of JAK1/JAK2 with IC50 of 11 nM/18 nM, ~10-fold selectivity versus JAK3. Momelotinib (CYT387) induces apoptosis and autophagy. Phase 3.
Condiciones de almacenamiento de almacenamiento
Store at -80°C
Enviado en
Dry ice packs + Cold packs
Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.
Grado
Moligand™
Tipo de acción
INHIBITOR
Mecanismo de acción
Tyrosine-protein kinase JAK2 inhibitor
Propiedades del producto
ALogP2.6
Nombres e identificadores
Isómeros SMILES C1COCCN1C2=CC=C(C=C2)NC3=NC=CC(=N3)C4=CC=C(C=C4)C(=O)NCC#N
Peso molecular 414.47
Reaxy-Rn 18462405
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18462405&ln=

Documentation

📋 Safety Data Sheet (SDS)

Comprehensive hazard, handling, storage, and regulatory compliance document.

Download SDS →

✅ Certificate of Analysis (COA)

Lot-specific quality data. Enter your lot number to retrieve the exact COA.

Look up COA →

📊 Datasheet

Quick-reference summary of product specifications and applications.

View datasheet →

🔬 Specification Sheet

Full quality attributes and acceptance criteria for this grade.

View spec sheet →

Advanced Data

Objetivos asociados (humanos)
JAK3 Tclin Tyrosine-protein kinase JAK3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK1 Tclin Tyrosine-protein kinase JAK1 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BMPR1B Tchem Bone morphogenetic protein receptor type-1B (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Tchem Uncharacterized protein FLJ45252 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ACVR1 Tchem Activin receptor type-1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
AAK1 Tchem AP2-associated protein kinase 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
OPA1 Tchem Dynamin-like 120 kDa protein, mitochondrial (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK2 Tclin Tyrosine-protein kinase JAK2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
Certificados (CoA, COO, BSE/TSE y tabla de análisis)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Propiedades químicas y físicas
SolubilidadSolubility (25°C) In vitro DMSO: 44 mg/mL (198.02 mM);    
Preguntas frecuentes y artículos
Calculadoras de soluciones
Reseñas

Reseñas de cliente

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