BLZ945 - CAS 953769-46-5
Catalog number:
953769-46-5
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C20H22N4O3S
Molecular Weight:
398.48
COA:
Inquire
Targets:
c-FMS
Description:
BLZ945 is an orally active, potent and selective CSF-1R inhibitor, which inhibits CSF-1R activity with an IC50 of 1nM and is more than 1000-fold selective against its closest receptor tyrosine kinase homologs c-KIT and Platelet-derived Growth Factor Receptor beta (PDGFRb).
Publictions citing BOC Sciences Products
  • >> More
Purity:
>98%
MSDS:
Inquire
1.Phenotypic and metabolic investigation of a CSF-1R kinase receptor inhibitor (BLZ945) and its pharmacologically active metabolite.
Krauser JA1, Jin Y, Walles M, Pfaar U, Sutton J, Wiesmann M, Graf D, Pflimlin-Fritschy V, Wolf T, Camenisch G, Swart P. Xenobiotica. 2015 Feb;45(2):107-23. doi: 10.3109/00498254.2014.945988. Epub 2014 Sep 2.
1. 4-[2((1R,2R)-2-Hydroxycyclohexylamino)-benzothiazol-6-yloxyl]-pyridine-2-carboxylic acid methylamide (BLZ945) is a small molecule inhibitor of CSF-1R kinase activity within osteoclasts designed to prevent skeletal related events in metastatic disease. Key metabolites were enzymatically and structurally characterized to understand the metabolic fate of BLZ945 and pharmacological implications. The relative intrinsic clearances for metabolites were derived from in vitro studies using human hepatocytes, microsomes and phenotyped with recombinant P450 enzymes. 2. Formation of a pharmacologically active metabolite (M9) was observed in human hepatocytes. The M9 metabolite is a structural isomer (diastereomer) of BLZ945 and is about 4-fold less potent. This isomer was enzymatically formed via P450 oxidation of the BLZ945 hydroxyl group, followed by aldo-keto reduction to the alcohol (M9). 3. Two reaction phenotyping approaches based on fractional clearances were applied to BLZ945 using hepatocytes and liver microsomes.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related c-FMS Products


CAS 873786-09-5 PLX-647

PLX-647
(CAS: 873786-09-5)

PLX-647 is PLX647 is a potent inhibitors of both FMS and KIT that show strong selectivity compared with other kinases. In the in vitro enzymatic assay, PLX647 i...

CAS 885704-21-2 c-FMS inhibitor

c-FMS inhibitor
(CAS: 885704-21-2)

c-FMS inhibitor is a novel c-Fms kinase inhibitor with a potential as anti-inflammatory agent and antirheumatic agent.

CAS 870483-87-7 GW2580

GW2580
(CAS: 870483-87-7)

GW2580 is an orally bioavailable inhibitor of cFMS kinase. GW2580 was found to completely inhibit human cFMS kinase in vitro at 0.06 microM and was inactive ag...

CAS 623142-96-1 Ki20227

Ki20227
(CAS: 623142-96-1)

Ki-20227 is a highly selective c-Fms tyrosine kinase(CSF1R) inhibitor.

CAS 1029044-16-3 Pexidartinib (PLX3397)

Pexidartinib (PLX3397)
(CAS: 1029044-16-3)

Pexidartinib (PLX3397) is an oral, potent mutil-targeted receptor tyrosine kinase inhibitor of CSF-1R with IC50 of 20 nM, Kit with IC50 of 10 nM, and Flt3 with ...

CAS 728033-96-3 OSI-930

OSI-930
(CAS: 728033-96-3)

OSI-930 is a selective thiophene-derived tyrosine kinase inhibitor with potential antineoplastic activity. Tyrosine kinase inhibitor OSI-930 inhibits stem cell ...

CAS 953769-46-5 BLZ945

BLZ945
(CAS: 953769-46-5)

BLZ945 is an orally active, potent and selective CSF-1R inhibitor, which inhibits CSF-1R activity with an IC50 of 1nM and is more than 1000-fold selective again...

Chemical Structure

CAS 953769-46-5 BLZ945

Quick Inquiry

Verification code

Featured Items