CDKI-73 - 95%, high purity , CAS No.1421693-22-2, Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 2;Inhibitor of cyclin dependent kinase 7;Inhibitor of cyclin dependent kinase 9

Item Number

C413829

• Synonyms: GAIOPWBQKZMUNO-UHFFFAOYSA-N | MS-26626 | 3-((5-fluoro-4-(4-methyl-2-(methylamino)thiazol-5-yl)pyrimidin-2-yl)amino)benzenesulfonamide | A925431 | GTPL12074 | 3,4-Dihydroxyphenylserine | AKOS030526509 | (+-)-1-(2-Piperidinyl)-2-propanone | 3-({5-fluoro-4-[
• Specifications & Purity: Moligand™, ≥95%
• Biochemical and Physiological Mechanisms: CDKI-73 (LS-007) is a potent CDK inhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficacious CDK9
• Storage Temp: Store at -20°C,Argon charged
• Shipped In: Ice chest + Ice pads
• Grade: Moligand™
• Action Type: INHIBITOR
• Mechanism of action: Inhibitor of cyclin dependent kinase 1;Inhibitor of cyclin dependent kinase 2;Inhibitor of cyclin dependent kinase 7;Inhibitor of cyclin dependent kinase 9

Product Description

Information

CDKI-73 (LS-007) is a potentCDKinhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficaciousCDK9inhibitor against acute myeloid leukemia.

Targets

CDK2 (Cell-free assay); CDK9 (Cell-free assay); CDK1 (Cell-free assay); CDK4 (Cell-free assay) 3.27 nM; 5.78 nM; 8.17 nM; 8.18 nM

In vitro

CDKI-73 induces cancer cells undergoing apoptosis through transcriptional downregulation of anti-apoptotic proteins Bcl-2, Mcl-1 and XIAP by majorly targeting CDK9. Contrastively, it is relatively low toxic to the bone marrow cells of healthy donors.

In vivo

CDKI-73 is orally bioavailable, highly efficacious against MLL-AML MV4–11 xenografts and downregulates anti-apoptotic proteins by targeting CDK9 in vivo.

Cell Research(from reference)

Cell lines：Leukemia cell lines (MOLM13, MV4-11, THP-1, etc.) 

Concentrations：0.05 μM, 0.1 μM, 0.25 μM, 0.5 μM 

Incubation Time：1 h, 4 h, 12 h, 24 h, 48 h