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Bosutinib (SKI-606) - Moligand™, 10mM in DMSO , Tyrosine-protein kinase Lyn inhibitor, CAS No.380843-75-4, Tyrosine-protein kinase Lyn inhibitor

CAS: 380843-75-4 Cat. No.: B407917 Peso molecular: 530.45 Número EC: 700-455-1
COA
Bosutinib (SKI-606) - Moligand™, 10mM in DMSO CAS No(380843-75-4) by Aladdin Scientific
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
4-(2,4-dichloro-5-methoxyphenylamino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile
Storage
Store at -80°C
Shipped In
Dry ice packs + Cold packs
★
 ·  off list, applied to all prices below.
Size
Estado
Price
Qty
1ml
B407917-1ml
1

105,90US$

153,90US$
Guardar 48,00 US$ (31.19%)
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SDS
Safety data
COA
Certificate
DS
Datasheet
SP
Spec sheet
Descripción general Specifications Propiedades del producto Nombres e identificadores Documentation Advanced Data Objetivos asociados (humanos) Certificados (CoA, COO, BSE/TSE y tabla de análisis) Propiedades químicas y físicas Calculadoras de soluciones Reseñas
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Why this grade

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

🌡

Storage & shipping

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

📋

Quality documents

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

📚

Literature proof

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

Descripción general

Information

Bosutinib (SKI-606) is a novel, dualSrc/Ablinhibitor withIC50of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity ofPI3K/AKT/mTOR,MAPK/ERKandJAK/STAT3signaling pathways by blocking the phosphorylation lev
In vitro

Bosutinib is selective for Src over non-Src family kinases with an IC50 of 1.2 nM, and potently inhibits Src-dependent cell proliferation with an IC50 of 100 nM. Bosutinib significantly inhibits the proliferation of Bcr-Abl-positive leukemia cell lines KU812, K562, and MEG-01 but not Molt-4, HL-60, Ramos, and other leukemia cell lines, with IC50 of 5 nM, 20 nM and 20 nM, respectively, more potently than that of STI-571. Similar to STI-571, Bosutinib displays antiproliferative activity against the Abl-MLV-transformed fibroblasts with IC50 of 90 nM. Bosutinib ablates tyrosine phosphorylation of Bcr-Abl and STAT5 in CML cells and of v-Abl expressed in fibroblasts at the concentration of ~50 nM, 10-25 nM and 200 nM, respectively, leading to the Bcr-Abl downstream signaling inhibition of Lyn/Hck phosphorylation. Although unable to inhibit the proliferation and survival of breast cancer cells, Bosutinib significantly decreases the motility and invasion of breast cancer cells with IC50 of ~250 nM, involved with an increase in cell-to-cell adhesion and membrane localization of β-catenin.

In vivo

Bosutinib (60 mg/kg/day) is active against Src-transformed fibroblasts xenografts and HT29 xenografts in nude mice with T/C of 18% and 30%, respectively. Oral administration of Bosutinib for 5 days significantly suppresses K562 tumor growth in mice in a dose-dependent manner, with the large tumors eradicated at dose of 100 mg/kg and tumor free at 150 mg/kg without overt toxicity. As being inactive against Colo205 xenografts in nude mice at 50 mg/kg twice daily, Bosutinib dosing at 75 mg/kg twice daily is necessary against Colo205 xenografts, and increasing the dose of Bosutinib has no additional benefit, in contrast to the significant dose-dependent ability against HT29 xenografts.
Cell Data

cell lines：Gli-Luc/MEF cells

Concentrations：Dissolved in DMSO, final concentrations ~1 μM

Incubation Time：72 hours

Powder Purity:≥98%

Specifications

Sinónimos
4-(2, 4-dichloro-5-methoxyphenylamino)-6-methoxy-7-(3-(4-methylpiperazin-1-yl)propoxy)quinoline-3-carbonitrile
Especificaciones y pureza
Moligand™, 10mM in DMSO
Mecanismos bioquímicos y fisiológicos
Bosutinib (SKI-606) is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphoryl
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 Lyn inhibitor
Propiedades del producto
ALogP5.4
Nombres e identificadores
Isómeros SMILES CN1CCN(CC1)CCCOC2=C(C=C3C(=C2)N=CC(=C3NC4=CC(=C(C=C4Cl)Cl)OC)C#N)OC
WGK Alemania 3
Peso molecular 530.45
Reaxy-Rn 9100307
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9100307&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)
CTH Tchem Cystathionine gamma-lyase (0 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHA2 Tclin Ephrin type-A receptor 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHA4 Tchem Ephrin type-A receptor 4 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHA8 Tchem Ephrin type-A receptor 8 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHB4 Tchem Ephrin type-B receptor 4 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ERBB4 Tclin Receptor tyrosine-protein kinase erbB-4 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHA5 Tchem Ephrin type-A receptor 5 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ERBB3 Tclin Receptor tyrosine-protein kinase erbB-3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EGFR Tclin Epidermal growth factor receptor (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHA3 Tchem Ephrin type-A receptor 3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SRC Tclin Proto-oncogene tyrosine-protein kinase Src (28 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
STK10 Tchem Serine/threonine-protein kinase 10 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
STK24 Tchem Serine/threonine-protein kinase 24 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
STK35 Tchem Serine/threonine-protein kinase 35 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
STK4 Tchem Serine/threonine-protein kinase 4 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TXK Tchem Tyrosine-protein kinase TXK (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
YES1 Tclin Tyrosine-protein kinase Yes (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FRK Tchem Tyrosine-protein kinase FRK (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FYN Tclin Tyrosine-protein kinase Fyn (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GAK Tchem Cyclin-G-associated kinase (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
FGR Tchem Tyrosine-protein kinase Fgr (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CAMK1D Tchem Calcium/calmodulin-dependent protein kinase type 1D (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SIK1 Tchem Serine/threonine-protein kinase SIK1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SIK2 Tchem Serine/threonine-protein kinase SIK2 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TNIK Tchem TRAF2 and NCK-interacting protein kinase (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SIK3 Tchem Serine/threonine-protein kinase SIK3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
SLK Tchem STE20-like serine/threonine-protein kinase (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PKMYT1 Tchem Membrane-associated tyrosine- and threonine-specific cdc2-inhibitory kinase (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MINK1 Tchem Misshapen-like kinase 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP2K2 Tclin Dual specificity mitogen-activated protein kinase kinase 2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP4K2 Tchem Mitogen-activated protein kinase kinase kinase kinase 2 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
LCK Tclin Tyrosine-protein kinase Lck (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP4K3 Tchem Mitogen-activated protein kinase kinase kinase kinase 3 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP4K4 Tchem Mitogen-activated protein kinase kinase kinase kinase 4 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP4K5 Tchem Mitogen-activated protein kinase kinase kinase kinase 5 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
LYN Tclin Tyrosine-protein kinase Lyn (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BTK Tclin Tyrosine-protein kinase BTK (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BMX Tchem Cytoplasmic tyrosine-protein kinase BMX (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BCR Tclin Breakpoint cluster region protein (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
BLK Tchem Tyrosine-protein kinase Blk (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
TNK2 Tclin Activated CDC42 kinase 1 (4 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL2 Tchem Tyrosine-protein kinase ABL2 (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL1 (23 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
HCK Tclin Tyrosine-protein kinase HCK (3 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
NTRK2 Tclin BDNF/NT-3 growth factors receptor (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
NTRK1 Tclin High affinity nerve growth factor receptor (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
CAMK2G Tchem Calcium/calmodulin-dependent protein kinase type II subunit gamma (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
MAP2K5 Tchem Dual specificity mitogen-activated protein kinase kinase 5 (1 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: 47 mg/mL (199.05 mM); Water: 47 mg/mL (199.05 mM); Ethanol: 10 mg/mL (42.35 mM);
Calculadoras de soluciones
Reseñas

Reseñas de cliente

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