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GSK1904529A - ≥98%, high purity , CAS No.1089283-49-7

In stock
Item Number
G127237
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SKU Size
Availability
Price Qty
G127237-5mg
5mg
2
$69.90
G127237-10mg
10mg
2
$109.90

Selective IGF-1R/IR tyrosine kinase inhibitor

Basic Description

Synonyms MOSKATHMXWSZTQ-UHFFFAOYSA-N | SB18897 | Trifluralin [ANSI:BSI:ISO] | AMY24202 | A24618 | GSK 4529 | IGF-1R inhibitor GS1904529A | MLS006010966 | N-(2,6-Difluorophenyl)-5-[3-[2-[[5-ethyl-2-(methyloxy)-4-[4-[4-(methylsulfonyl)-1-piperazinyl]-1-Piperidinyl]p
Specifications & Purity Moligand™, ≥98%
Biochemical and Physiological Mechanisms GSK1904529A, which potently inhibits IGF-IR (IC50= 27 nmol/L) and IR (IC50= 25 nmol/L) activities in vitro and in vivo, is a promising candidate for therapeutic use in solid and hematologic cancers.Selective IGF-1R (IC 50 = 27 nM in cell) and Insulin Rece
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Note Refer to SDS for further information. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.
Product Description

GSK1904529A is a potent, selective, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity.

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Benzenoids
Class Benzene and substituted derivatives
Subclass Anilides
Intermediate Tree Nodes Aromatic anilides
Direct Parent Benzanilides
Alternative Parents Phenylpiperidines  Phenylimidazoles  Aminophenyl ethers  Benzamides  Imidazo[1,2-a]pyridines  Imidazopyridines  Methoxyanilines  Phenoxy compounds  Anisoles  Benzoyl derivatives  Dialkylarylamines  Methoxybenzenes  Fluorobenzenes  Alkyl aryl ethers  Aminopiperidines  N-alkylpiperazines  Aminopyrimidines and derivatives  Pyridines and derivatives  Organosulfonamides  Aryl fluorides  Organic sulfonamides  N-substituted imidazoles  Sulfonyls  Heteroaromatic compounds  Amino acids and derivatives  Secondary carboxylic acid amides  Trialkylamines  Azacyclic compounds  Secondary amines  Organofluorides  Organopnictogen compounds  Hydrocarbon derivatives  Organic oxides  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Benzanilide - Phenylpiperidine - 4-phenylimidazole - 5-phenylimidazole - Aminophenyl ether - Imidazopyridine - Methoxyaniline - Benzoic acid or derivatives - Benzamide - Imidazo[1,2-a]pyridine - Methoxybenzene - Aniline or substituted anilines - Dialkylarylamine - Benzoyl - Phenol ether - Tertiary aliphatic/aromatic amine - Anisole - Phenoxy compound - Alkyl aryl ether - 4-aminopiperidine - Fluorobenzene - N-alkylpiperazine - Halobenzene - Aminopyrimidine - Aryl fluoride - Aryl halide - 1,4-diazinane - N-substituted imidazole - Organosulfonic acid amide - Organic sulfonic acid amide - Piperazine - Piperidine - Pyridine - Pyrimidine - Sulfonyl - Organic sulfonic acid or derivatives - Azole - Organosulfonic acid or derivatives - Heteroaromatic compound - Imidazole - Secondary carboxylic acid amide - Tertiary amine - Tertiary aliphatic amine - Amino acid or derivatives - Carboxamide group - Secondary amine - Organoheterocyclic compound - Ether - Carboxylic acid derivative - Azacycle - Organosulfur compound - Organic oxygen compound - Hydrocarbon derivative - Organopnictogen compound - Organohalogen compound - Organic oxide - Organic nitrogen compound - Amine - Organofluoride - Organonitrogen compound - Organooxygen compound - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as benzanilides. These are aromatic compounds containing an anilide group in which the carboxamide group is substituted with a benzene ring. They have the general structure RNC(=O)R', where R,R'= benzene.
External Descriptors Not available

Associated Targets(Human)

IGF1R Tclin Insulin-like growth factor 1 receptor (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
INSR Tclin Insulin receptor (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
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
MAPK14 Tchem MAP kinase p38 alpha (12866 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKB Tchem Serine/threonine-protein kinase Aurora-B (6805 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ERBB4 Tclin Receptor protein-tyrosine kinase erbB-4 (2748 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
YES1 Tclin Tyrosine-protein kinase YES (2781 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 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
U2OS (164939 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
A549 (127892 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HFF (3142 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRAF Tclin Serine/threonine-protein kinase B-raf (11587 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LP-1 (136 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK-293T (167025 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
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Canis familiaris (36305 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Cynomolgus monkey (4946 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

Mechanisms of Action

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

Names and Identifiers

Pubchem Sid 504769975
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504769975
IUPAC Name N-(2,6-difluorophenyl)-5-[3-[2-[5-ethyl-2-methoxy-4-[4-(4-methylsulfonylpiperazin-1-yl)piperidin-1-yl]anilino]pyrimidin-4-yl]imidazo[1,2-a]pyridin-2-yl]-2-methoxybenzamide
INCHI InChI=1S/C44H47F2N9O5S/c1-5-28-26-35(38(60-3)27-36(28)53-19-15-30(16-20-53)52-21-23-54(24-22-52)61(4,57)58)49-44-47-17-14-34(48-44)42-40(50-39-11-6-7-18-55(39)42)29-12-13-37(59-2)31(25-29)43(56)51-41-32(45)9-8-10-33(41)46/h6-14,17-18,25-27,30H,5,15-16,19-24H2,1-4H3,(H,51,56)(H,47,48,49)
InChIKey MOSKATHMXWSZTQ-UHFFFAOYSA-N
Smiles CCC1=CC(=C(C=C1N2CCC(CC2)N3CCN(CC3)S(=O)(=O)C)OC)NC4=NC=CC(=N4)C5=C(N=C6N5C=CC=C6)C7=CC(=C(C=C7)OC)C(=O)NC8=C(C=CC=C8F)F
Isomeric SMILES CCC1=CC(=C(C=C1N2CCC(CC2)N3CCN(CC3)S(=O)(=O)C)OC)NC4=NC=CC(=N4)C5=C(N=C6N5C=CC=C6)C7=CC(=C(C=C7)OC)C(=O)NC8=C(C=CC=C8F)F
Molecular Weight 851.96
Reaxy-Rn 18680285
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=18680285&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.

2 results found

Lot Number Certificate Type Date Item
I2214754 Certificate of Analysis Jun 17, 2024 G127237
I2214752 Certificate of Analysis Jun 17, 2024 G127237

Chemical and Physical Properties

Solubility DMSO 124 mg/mL Water <1 mg/mL Ethanol <1 mg/mL
Molecular Weight 852.000 g/mol
XLogP3 6.800
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 14
Rotatable Bond Count 12
Exact Mass 851.339 Da
Monoisotopic Mass 851.339 Da
Topological Polar Surface Area 155.000 Ų
Heavy Atom Count 61
Formal Charge 0
Complexity 1530.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
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

Citations of This Product

1. Majid Manzoor, Danni Chen, Jiahui Lin, Ying Wang, Lan Xiang, Jianhua Qi.  (2025)  Isoquercitrin promotes hair growth through induction of autophagy and angiogenesis by targeting AMPK and IGF-1R.  PHYTOMEDICINE,  136  (156289). 

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