Shelf life (days): 1460.0
Formulation: A crystalline solid
Formal Name: 8-cyclopentyl-2-[2-[4-(3,4-dihydro-5,7-dimethoxy-4-oxo-2-quinazolinyl)benzoyl]-2,7-diazaspiro[3.5]non-7-yl]-5-methyl-pyrido[2,3-d]pyrimidin-7(8H)-one
Purity: ≥98%
Formula Markup: C37H39N7O5
Formula Weight: 661.763
CAS Number: 3036645-03-8
Notes: A dual inhibitor of Cdk6 and BRD4 (IC50s = 36.03, 234.12, and 137.42 nM for Cdk6 and BRD4 BD1 and BD2, respectively); selective for Cdk6 over Cdk1-Cdk5 at 500 nM; selective for BD1 and BD2 in BRD4 over those in BRD2 and BRD3 (IC50s = >1,000, >1,000, 863.41, and 967.5 nM, respectively); inhibits the proliferation of MDA-MB-231 and BT-549 TNBC cells (IC50s = 2,250 and 980 nM, respectively) but not non-cancerous MCF-10A cells (IC50 = >16.1 µM); synergistically reduces colony formation of MDA-MB-231 cells at 2 µM in combination with RSL3; reduces tumor growth in an MDA-MB-231 mouse xenograft model at 25 mg/kg every other day
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