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Belizatinib (TSR-011) - 98%, 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

Moligand™
≥98%

CAS#: 1357920-84-3
Formula: C₃₃H₄₄FN₅O₃
Molecular Weight: 577.73
PubChem CID: 57345941

Item Number

B414037

Grouped product items
SKU	Size	Availability	Price
B414037-5mg	5mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$107.90
B414037-25mg	25mg	Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding.	$347.90
B414037-100mg	100mg	In stock	$663.90

TrkA Selective Inhibitors

View related series

ALK receptor tyrosine kinase Inhibitor AXL receptor tyrosine kinase Inhibitor fms related receptor tyrosine kinase 3 Inhibitor interleukin 1 receptor associated kinase 1 Inhibitor LCK proto-oncogene，Src family tyrosine kinase Inhibitor leukocyte receptor tyrosine kinase Inhibitor MER proto-oncogene，tyrosine kinase Inhibitor mitogen-activated protein kinase kinase kinase kinase 2 Inhibitor

Basic Description

Synonyms	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
Specifications & Purity	Moligand™, ≥98%
Biochemical and Physiological Mechanisms	"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)."
Storage Temp	Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	INHIBITOR
Mechanism of 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.

ALogP

4.827

HBD Count

Rotatable Bond

Associated Targets

IRAK1 Tchem Interleukin-1 receptor-associated kinase 1 0 Activities

Discover Target: IRAK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MERTK Tchem Tyrosine-protein kinase Mer 0 Activities

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Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAP4K2 Tchem Mitogen-activated protein kinase kinase kinase kinase 2 0 Activities

Discover Target: MAP4K2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

LCK Tclin Tyrosine-protein kinase Lck 0 Activities

Discover Target: LCK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

LTK Tclin Leukocyte tyrosine kinase receptor 0 Activities

Discover Target: LTK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ALK Tclin ALK tyrosine kinase receptor 0 Activities

Discover Target: ALK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AXL Tchem Tyrosine-protein kinase receptor UFO 0 Activities

Discover Target: AXL

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

INSR Tclin Insulin receptor 0 Activities

Discover Target: INSR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NTRK2 Tclin BDNF/NT-3 growth factors receptor 0 Activities

Discover Target: NTRK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NTRK1 Tclin High affinity nerve growth factor receptor 0 Activities

Discover Target: NTRK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NTRK3 Tclin NT-3 growth factor receptor 0 Activities

Discover Target: NTRK3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

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)
InChi Key	WSTUJEXAPHIEIM-UHFFFAOYSA-N
Canonical 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
Isomeric 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
PubChem CID	57345941
Molecular Weight	577.73

CAS Registry No.

PubChem CID

ChEMBL Ligand

BindingDB Ligand

RCSB PDB Ligand

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Lot Number	Certificate Type	Date	Item
F2222269	Certificate of Analysis	Jun 01, 2022	B414037

Solubility

Solubility (25°C) In vitro DMSO: 100 mg/mL (173.09 mM); Ethanol: 100 mg/mL (173.09 mM); Water: Insoluble;

DMSO(mg / mL) Max Solubility

100

DMSO(mM) Max Solubility

173.0912364

Water(mg / mL) Max Solubility

＜1

References

1. Lewis RT, Bode CM, Choquette DM, Potashman M, Romero K, Stellwagen JC, Teffera Y, Moore E, Whittington DA, Chen H et al.. (2012) The discovery and optimization of a novel class of potent, selective, and orally bioavailable anaplastic lymphoma kinase (ALK) inhibitors with potential utility for the treatment of cancer.. J Med Chem, 55 (14): (6523-40). [PMID:22734674]

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