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BMS-536924 - ≥98%, high purity , CAS No.468740-43-4, Inhibitor of CYP3A4;Inhibitor of Insulin-like growth factor I receptor;Inhibitor of Insulin receptor

In stock
Item Number
B126005
Grouped product items
SKU Size
Availability
Price Qty
B126005-1mg
1mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$31.90
B126005-5mg
5mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$69.90
B126005-25mg
25mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$245.90
B126005-100mg
100mg
Available within 8-12 weeks(?)
Production requires sourcing of materials. We appreciate your patience and understanding.
$629.90

Dual IR/IGF1R inhibitor

Basic Description

Synonyms HY-10262 | N6I | 4-{[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino}-3-[7-methyl-5-(morpholin-4-yl)-1H-1,3-benzodiazol-2-yl]-1,2-dihydropyridin-2-one | CHEBI:91454 | NSC761760 | NSC-761760 | BCP02116 | MLS006011171 | BMS-536924, >=98% (HPLC) | D94990
Specifications & Purity Moligand™, ≥98%
Biochemical and Physiological Mechanisms Dual inhibitor of the insulin receptor (IR) and insulin-like growth factor-1 receptor (IGF1R) (IC50values are 73 and 100 nM respectively). Inhibits receptor autophosphorylation and downstream MEK1/2 and Akt signaling. Induces G1arrest and apoptosis in ML-
Storage Temp Store at -20°C,Argon charged
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action Inhibitor of CYP3A4;Inhibitor of Insulin-like growth factor I receptor;Inhibitor of Insulin receptor

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organoheterocyclic compounds
Class Benzimidazoles
Subclass Not available
Intermediate Tree Nodes Not available
Direct Parent Benzimidazoles
Alternative Parents Dialkylarylamines  Secondary alkylarylamines  Pyridinones  Chlorobenzenes  Aminopyridines and derivatives  Dihydropyridines  Aralkylamines  Aryl chlorides  Morpholines  Vinylogous amides  Imidazoles  Heteroaromatic compounds  Secondary alcohols  1,2-aminoalcohols  Lactams  Dialkyl ethers  Azacyclic compounds  Oxacyclic compounds  Aromatic alcohols  Hydrocarbon derivatives  Organic oxides  Organochlorides  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Benzimidazole - Tertiary aliphatic/aromatic amine - Dialkylarylamine - Dihydropyridine - Halobenzene - Chlorobenzene - Pyridinone - Secondary aliphatic/aromatic amine - Aminopyridine - Aralkylamine - Aryl halide - Aryl chloride - Morpholine - Monocyclic benzene moiety - Oxazinane - Pyridine - Hydropyridine - Benzenoid - Heteroaromatic compound - Vinylogous amide - Imidazole - Azole - 1,2-aminoalcohol - Secondary alcohol - Lactam - Tertiary amine - Oxacycle - Azacycle - Ether - Secondary amine - Dialkyl ether - Organic nitrogen compound - Organohalogen compound - Organochloride - Organonitrogen compound - Organooxygen compound - Aromatic alcohol - Hydrocarbon derivative - Organic oxide - Organic oxygen compound - Amine - Alcohol - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as benzimidazoles. These are organic compounds containing a benzene ring fused to an imidazole ring (five member ring containing a nitrogen atom, 4 carbon atoms, and two double bonds).
External Descriptors Not available

Associated Targets(Human)

CYP3A4 Tclin Cytochrome P450 3A4 (5 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
CSF1R Tclin Macrophage colony-stimulating factor 1 receptor (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
RET Tclin Proto-oncogene tyrosine-protein kinase receptor Ret (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
SRC Tclin Proto-oncogene tyrosine-protein kinase Src (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ROS1 Tclin Proto-oncogene tyrosine-protein kinase ROS (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FRK Tchem Tyrosine-protein kinase FRK (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FYN Tclin Tyrosine-protein kinase Fyn (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PTK2B Tclin Protein-tyrosine kinase 2-beta (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
IGF1R Tclin Insulin-like growth factor 1 receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PLK4 Tchem Serine/threonine-protein kinase PLK4 (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
SYK Tclin Tyrosine-protein kinase SYK (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
LYN Tclin Tyrosine-protein kinase Lyn (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
BLK Tchem Tyrosine-protein kinase Blk (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AXL Tchem Tyrosine-protein kinase receptor UFO (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
INSR Tclin Insulin receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
NTRK2 Tclin BDNF/NT-3 growth factors receptor (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
NTRK1 Tclin High affinity nerve growth factor receptor (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
NTRK3 Tclin NT-3 growth factor receptor (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
JAK2 Tclin Tyrosine-protein kinase JAK2 (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
EGFR Tclin Epidermal growth factor receptor erbB1 (33727 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
INSR Tclin Insulin receptor (5558 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ERBB2 Tclin Receptor protein-tyrosine kinase erbB-2 (7851 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IGF1R Tclin Insulin-like growth factor I receptor (8605 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LCK Tclin Tyrosine-protein kinase LCK (9212 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KDR Tclin Vascular endothelial growth factor receptor 2 (20924 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PTK2 Tclin Focal adhesion kinase 1 (4730 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP2K1 Tclin Dual specificity mitogen-activated protein kinase kinase 1 (4127 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MET Tclin Hepatocyte growth factor receptor (10718 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NR1I2 Tchem Pregnane X receptor (6667 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AKT1 Tchem Serine/threonine-protein kinase AKT (9192 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
STK4 Tchem Serine/threonine-protein kinase MST1 (2643 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
A498 (42825 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BT-474 (2113 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
C8166 (1658 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CA46 (271 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Calu-6 (398 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CCRF-CEM (65223 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
COLO 205 (50209 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Daudi (625 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
DMS-79 (150 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
EVSA-T (142 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HL-60 (67320 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HuTu80 (255 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IM-9 (160 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JAR (316 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
JIYOYE (162 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
K562 (73714 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
KM12 (47707 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MCF7 (126967 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ML-2 (146 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MOLT-4 (49676 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NALM-6 (592 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NCI-H128 (54 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NCI-H345 (89 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NTERA-2-cl-D1 (234 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
OVCAR-4 (44535 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PSN1 (345 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Raji (5516 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RD (1212 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RKO (1376 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RPMI-8226 (44974 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
RXF 393 (41971 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SCC-15 (194 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
SF-126 (160 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Igf1r Insulin-like growth factor 1 receptor (35 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasma (328 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Serum (58 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

IUPAC Name 4-[[(2S)-2-(3-chlorophenyl)-2-hydroxyethyl]amino]-3-(4-methyl-6-morpholin-4-yl-1H-benzimidazol-2-yl)-1H-pyridin-2-one
INCHI InChI=1S/C25H26ClN5O3/c1-15-11-18(31-7-9-34-10-8-31)13-20-23(15)30-24(29-20)22-19(5-6-27-25(22)33)28-14-21(32)16-3-2-4-17(26)12-16/h2-6,11-13,21,32H,7-10,14H2,1H3,(H,29,30)(H2,27,28,33)/t21-/m1/s1
InChIKey ZWVZORIKUNOTCS-OAQYLSRUSA-N
Smiles CC1=CC(=CC2=C1N=C(N2)C3=C(C=CNC3=O)NCC(C4=CC(=CC=C4)Cl)O)N5CCOCC5
Isomeric SMILES CC1=CC(=CC2=C1N=C(N2)C3=C(C=CNC3=O)NC[C@H](C4=CC(=CC=C4)Cl)O)N5CCOCC5
Molecular Weight 479.97
Reaxy-Rn 11849297
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=11849297&ln=

Certificates(CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

9 results found

Lot Number Certificate Type Date Item
E2514127 Certificate of Analysis Apr 18, 2025 B126005
E2514160 Certificate of Analysis Apr 18, 2025 B126005
E2514161 Certificate of Analysis Apr 18, 2025 B126005
E2514162 Certificate of Analysis Apr 18, 2025 B126005
E2514163 Certificate of Analysis Apr 18, 2025 B126005
E2514164 Certificate of Analysis Apr 18, 2025 B126005
E2514165 Certificate of Analysis Apr 18, 2025 B126005
E2514166 Certificate of Analysis Apr 18, 2025 B126005
E2514167 Certificate of Analysis Apr 18, 2025 B126005

Chemical and Physical Properties

Solubility Solvent:DMSO, Max Conc. mg/mL: 48, Max Conc. mM: 100
Sensitivity light & Moisture sensitive
Molecular Weight 480.000 g/mol
XLogP3 2.700
Hydrogen Bond Donor Count 4
Hydrogen Bond Acceptor Count 6
Rotatable Bond Count 6
Exact Mass 479.172 Da
Monoisotopic Mass 479.172 Da
Topological Polar Surface Area 103.000 Ų
Heavy Atom Count 34
Formal Charge 0
Complexity 801.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 1
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Solution Calculators

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