UM-164 – 5 mg

Brand:
Cayman
CAS:
903564-48-7
Storage:
-20
UN-No:
Non-Hazardous - /

UM-164 is an inhibitor of Src and p38 MAPK kinases (Kds = 2.7, 2.2, and 5.5 nM for c-Src, p38α, and p38β, respectively).{48199} It also inhibits Fyn, Yes, Lyn, Abl, Arg, Ack, Csk, EphB2, EphB4, and Zak by greater than 75% in a kinome profiling assay using MDA-MB-231 cell lysates when used at a concentration of 500 nM. UM-164 inhibits cell growth in a panel of triple-negative breast cancer (TNBC) cell lines (IC50s = 6.1-260 nM) and in a patient-derived TNBC cell line (IC50 = 320 nM). In MDA-MB-231 and SUM149 cells, UM-164 (1 μM) induces cell cycle arrest at the G1/S phase and inhibits cell motility and invasion when used at concentrations greater than or equal to 50 nM. UM-164 (≥10 mg/kg) reduces tumor growth in SUM149 and MDA-MB-231 mouse xenograft models.  

 

Available on backorder

SKU: 26188 - 5 mg Category:

Description

An inhibitor of Src and p38 MAPK kinases (Kds = 2.7, 2.2, and 5.5 nM for c-Src, p38α, and p38β, respectively); also inhibits Fyn, Yes, Lyn, Abl, Arg, Ack, Csk, EphB2, EphB4, and Zak at 500 nM; inhibits cell growth in a panel of TNBC cell lines (IC50s = 6.1-260 nM) and in a patient-derived TNBC cell line (IC50 = 320 nM); induces cell cycle arrest at the G1/S phase MDA-MB-231 and SUM149 cells at 1 μM; inhibits cell motility and invasion in MDA-MB-231 and SUM149 cells at ≥ 50 nM; reduces tumor growth in SUM149 and MDA-MB-231 mouse xenograft models at ≥10 mg/kg


Formal name: 2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-N-[2-methyl-5-[[3-(trifluoromethyl)benzoyl]amino]phenyl]-5-thiazolecarboxamide

Synonyms: 

Molecular weight: 640.7

CAS: 903564-48-7

Purity: ≥98%

Formulation: A crystalline solid


Product Type|Biochemicals|Kinase Inhibitors|p38 MAPK||Product Type|Biochemicals|Kinase Inhibitors|SRC Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Cycle|G1||Research Area|Cancer|Cell Migration & Metastasis||Research Area|Cancer|Cell Signaling|Abl family & Bcr-Abl Signaling||Research Area|Cancer|Cell Signaling|SRC Family Signaling