SML2822
AZ12601011
≥98% (HPLC)
Synonym(e):
1-(2-Pyridin-2-yl-6,7dihydro-5H-cyclopenta[e]pyrimidin-4-yl)pyrrolo[3,2-c]pyridine, 2-(2-Pyridinyl)-4-(1H-pyrrolo[3,2-c]pyridin-1-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidine, AZ 12601011, AZ-12601011
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Empirische Formel (Hill-System):
C19H15N5
Molekulargewicht:
313.36
NACRES:
NA.77
UNSPSC Code:
12352200
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Unterstützung erhaltenassay
≥98% (HPLC)
form
powder
color
white to light brown
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
Verwandte Kategorien
Biochem/physiol Actions
AZ12601011 is an orally active, subtype-selective TGF-β type I receptors active site inhibitor (active-site affinity: ALK4/5/6 Kd = 2.6/2.9/42 nM, ALK1/2/3 Kd = 40/15/40 μM) that prevents ALK4/5/7-mediated Smad2, but not ALK1/2/3/6-mediated Smad1, phosphorylation (10 μM; NIH3T3 expressing respective constitutively active receptors). AZ12601011 inhibits 4T1 murine mammary carcinoma growth in cultures (IC50 = 400 nM) and in vivo (50 mg/kg bid. po. mice). AZ12601011 also causes heart valve lesions and physeal dysplasia in rats (150 mg/kg/day po. for 7 days), consistent with a critical role of ALK5 in maintaining the integrity of heart valve and physis.
Orally active, subtype-selective TGF-β type I receptors ALK4/5/7 active site inhibitor in vitro and in vivo.
Lagerklasse
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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