Asciminib – 5 mg

Brand:
Cayman
CAS:
1492952-76-7
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Asciminib is an allosteric inhibitor of Abl1 (IC50 = 0.45 nM).{43921} It is selective for Abl1 over a panel of more than 60 additional kinases (IC50s = >10 μM), as well as ion channels, nuclear receptors, G protein-coupled receptors (GPCRs), and transporters. Asciminib inhibits the proliferation of Luc-Ba/F3 cells transformed with wild-type Bcr-Abl1 or the drug-resistant mutant Bcr-Abl1T315I (GI50s = 1 and 25 nM, respectively), as well as other drug-resistant mutants.{43922} It reduces tumor growth in a KCL-22 chronic myelogenous leukemia (CML) mouse xenograft model when administered at a dose of 3 mg/kg twice per day and induces tumor regression at doses of greater than or equal to 7.5 mg/kg twice per day.  

 

Available on backorder

SKU: 26126 - 5 mg Category:

Description

An allosteric inhibitor of Abl1 (IC50 = 0.45 nM); selective for Abl1 over a panel of more than 60 additional kinases (IC50s = >10 μM), as well as ion channels, nuclear receptors, GPCRs, and transporters; inhibits the proliferation of Luc-Ba/F3 cells transformed with wild-type Bcr-Abl1 or the drug-resistant mutant Bcr-Abl1T315I (GI50s = 1 and 25 nM, respectively), as well as other drug-resistant mutants; reduces tumor growth in a KCL-22 CML mouse xenograft model at 3 mg/kg twice per day and induces tumor regression at ≥7.5 mg/kg twice per day


Formal name: N-[4-(chlorodifluoromethoxy)phenyl]-6-[(3R)-3-hydroxy-1-pyrrolidinyl]-5-(1H-pyrazol-3-yl)-3-pyridinecarboxamide

Synonyms:  ABL001

Molecular weight: 449.8

CAS: 1492952-76-7

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Kinase Inhibitors|Abl Family & Bcr-Abl||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Abl family & Bcr-Abl Signaling