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Key Documents

SML2822

Sigma-Aldrich

AZ12601011

≥98% (HPLC)

Synonyma:

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

Přihlásitk zobrazení cen stanovených pro organizaci a smluvních cen


About This Item

Empirický vzorec (Hillův zápis):
C19H15N5
Molekulová hmotnost:
313.36
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

assay

≥98% (HPLC)

form

powder

color

white to light brown

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

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.

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable


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