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Belizatinib (TSR-011) - 10mM in DMSO, high purity , CAS No.1357920-84-3, Inhibitor of ALK receptor tyrosine kinase;Inhibitor of AXL receptor tyrosine kinase;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of interleukin 1 receptor associated kinase 1;Inhibitor of LCK proto-oncogene; Src family tyrosine kinase;Inh

COA COA
En stock
Item Number
B421361
Articles du produit groupé
SKU Taille
Disponibilité
 Prix Qté
B421361-1ml
1ml
Available within 8-12 weeks(?)
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241,90$US
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TrkA Selective Inhibitors

View related series
Compound libraries (12325) Receptor Tyrosine Kinase (1260)

Description générale

Synonymes Belizatinib | 1357920-84-3 | TSR-011 | Belizatinib (TSR011) | Belizatinib [INN] | Belizatinib [WHO-DD] | Belizatinib(TSR-011) | CHEMBL2172308 | Z8A6022P3J | 4-fluoro-N-(6-((4-(2-hydroxypropan-2-yl)piperidin-1-yl)methyl)-1-((1s,4s)-4-(isopropylcarbamoyl)cyclohexyl)-1H-benzo
Spécifications et pureté Moligand™, 10mM in DMSO
Mécanismes biochimiques et physiologiques "Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C)."
Température de stockage Store at -80°C
Expédié en
Ice chest + Ice pads
Ce produit nécessite l'expédition en chaîne froide. Les services terrestres et autres services économiques ne sont pas disponibles.
Grade Moligand™
Type d'action INHIBITOR
Mécanisme d'action Inhibitor of ALK receptor tyrosine kinase;Inhibitor of AXL receptor tyrosine kinase;Inhibitor of fms related receptor tyrosine kinase 3;Inhibitor of interleukin 1 receptor associated kinase 1;Inhibitor of LCK proto-oncogene; Src family tyrosine kinase;Inh
Product Description

Information

"Belizatinib (TSR-011) is a potent inhibitor ofALK(IC50=0.7 nM) andtropomyosin receptor kinase (TRK)(IC50 values less than 3 nM for TRK A, B, and C). "

Targets

TrkA ; TrkB ; TrkC ; TrkA ; TrkB 28040,;

In vitro

TSR-011 has high affinity for wild-type recombinant ALK kinase activity, with an IC50 value of 0.7\u2009nM and inhibits tropomyosin receptor kinase (TRK) A, B, and C (IC50 < 3nM).

In vivo

TSR-011 exerts sustained potent inhibition of ALK-dependent tumour growth in mouse models. It is well-tolerated.

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Benzenoids
Classe Benzene and substituted derivatives
Subclass Benzoic acids and derivatives
Intermediate Tree Nodes Halobenzoic acids and derivatives
Direct Parent 4-halobenzoic acids and derivatives
Alternative Parents Benzamides  Benzimidazoles  Benzoyl derivatives  Aralkylamines  Fluorobenzenes  Aryl fluorides  Piperidines  N-substituted imidazoles  Tertiary alcohols  Heteroaromatic compounds  Secondary carboxylic acid amides  Amino acids and derivatives  Trialkylamines  Azacyclic compounds  Carbonyl compounds  Organic oxides  Organofluorides  Hydrocarbon derivatives  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents 4-halobenzoic acid or derivatives - Benzamide - Benzimidazole - Benzoyl - Aralkylamine - Fluorobenzene - Halobenzene - Aryl fluoride - Aryl halide - Piperidine - N-substituted imidazole - Azole - Heteroaromatic compound - Tertiary alcohol - Imidazole - Amino acid or derivatives - Carboxamide group - Tertiary aliphatic amine - Tertiary amine - Secondary carboxylic acid amide - Carboxylic acid derivative - Organoheterocyclic compound - Azacycle - Alcohol - Amine - Carbonyl group - Hydrocarbon derivative - Organic oxide - Organic oxygen compound - Organic nitrogen compound - Organooxygen compound - Organohalogen compound - Organofluoride - Organonitrogen compound - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as 4-halobenzoic acids and derivatives. These are benzoic acids or derivatives carrying a halogen atom at the 4-position of the benzene ring.
External Descriptors Not available

Propriétés du produit

ALogP 4.827
hba_count 3
Nombre de HBD 2
Liaison rotative 7

Cibles associées (humaines)

IRAK1 Tchem Interleukin-1 receptor-associated kinase 1 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (0 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MERTK Tchem Tyrosine-protein kinase Mer (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
MAP4K2 Tchem Mitogen-activated protein kinase kinase kinase kinase 2 (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
LCK Tclin Tyrosine-protein kinase Lck (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
LTK Tclin Leukocyte tyrosine kinase receptor (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ALK Tclin ALK tyrosine kinase receptor (4 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
AXL Tchem Tyrosine-protein kinase receptor UFO (1 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
INSR Tclin Insulin receptor (5558 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
NTRK1 Tclin Nerve growth factor receptor Trk-A (7922 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
FLT3 Tclin Tyrosine-protein kinase receptor FLT3 (13481 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
IRAK1 Tchem Interleukin-1 receptor-associated kinase 1 (1749 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HepG2 (196354 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AXL Tchem Tyrosine-protein kinase receptor UFO (3469 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NTRK2 Tclin Neurotrophic tyrosine kinase receptor type 2 (3279 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
ALK Tclin ALK tyrosine kinase receptor (7132 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MAP4K2 Tchem Mitogen-activated protein kinase kinase kinase kinase 2 (2692 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MERTK Tchem Proto-oncogene tyrosine-protein kinase MER (2687 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
NTRK3 Tclin NT-3 growth factor receptor (2338 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
LTK Tclin Leukocyte tyrosine kinase receptor (1542 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Liver microsomes (16955 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Liver (3974 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Cibles associées (non humaines)

Canis familiaris (36305 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
Rattus norvegicus (775804 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
Liver microsome (341 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mécanismes d'action

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

Noms et identifiants

IUPAC Name 4-fluoro-N-[6-[[4-(2-hydroxypropan-2-yl)piperidin-1-yl]methyl]-1-[4-(propan-2-ylcarbamoyl)cyclohexyl]benzimidazol-2-yl]benzamide
INCHI InChI=1S/C33H44FN5O3/c1-21(2)35-30(40)24-8-12-27(13-9-24)39-29-19-22(20-38-17-15-25(16-18-38)33(3,4)42)5-14-28(29)36-32(39)37-31(41)23-6-10-26(34)11-7-23/h5-7,10-11,14,19,21,24-25,27,42H,8-9,12-13,15-18,20H2,1-4H3,(H,35,40)(H,36,37,41)
InChIKey WSTUJEXAPHIEIM-UHFFFAOYSA-N
Smiles CC(C)NC(=O)C1CCC(CC1)N2C3=C(C=CC(=C3)CN4CCC(CC4)C(C)(C)O)N=C2NC(=O)C5=CC=C(C=C5)F
Isomères SMILES CC(C)NC(=O)C1CCC(CC1)N2C3=C(C=CC(=C3)CN4CCC(CC4)C(C)(C)O)N=C2NC(=O)C5=CC=C(C=C5)F
Poids moléculaire 577.73
Reaxy-Rn 39603420
Reaxys-RN_link_address https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=39603420&ln=

Certificats (CoA, COO, BSE/TSE et tableau d'analyse)

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

Propriétés chimiques et physiques

DMSO (mg/mL) Solubilité maximale 100
DMSO (mM) Solubilité maximale 173.0912364
Eau (mg/mL) Solubilité maximale ＜1
Poids moléculaire 577.700 g/mol
XLogP3 4.500
Hydrogen Bond Donor Count 3
Hydrogen Bond Acceptor Count 6
Rotatable Bond Count 8
Exact Mass 577.343 Da
Monoisotopic Mass 577.343 Da
Topological Polar Surface Area 99.500 Ų
Heavy Atom Count 42
Formal Charge 0
Complexity 909.000
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

Calculateurs de solution

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