SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a K D of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (K i =2600 nM), CDK9 (K i =960 nM), CDK12 (K i =870 nM). SY-5609 induces apoptosis in tumor cells and has a
Storage Temp
Store at 2-8°C
Shipped In
Wet ice
Product Description
SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a K D of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (K i =2600 nM), CDK9 (K i =960 nM), CDK12 (K i =870 nM). SY-5609 induces apoptosis in tumor cells and has antitumor activity
In Vitro
SY-5609 (0.01-10000 nM; 72 hours) demonstrates strong antiproliferative effects in triple negative breast cancer (TNBC) and ovarian (OVA) cancer cells. SY-5609 (100-500 nM; 48, 72 hours) induces apoptosis. SY-5609 (100-500 nM; 48 hours) induces G2/M cell cycle arrest in HCC70 cells. SY-5609 (25-500 nM; 6-48 hours) results in inhibition of the phosphorylation of CDK2 at Thr160 via loss of CAK function for 24 and 48 h. SY-5609 (compound 101; 126.4 pM-4 µM; 72 hours) has an EC 50 of 5.6 nM in HCC70 cell line. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: HCC70, MDA-MB453, COV504, A2780, OVCAR3, CAOV3 cells Concentration: 0.01-10000 nM Incubation Time: 72 hours Result: Demonstrated strong antiproliferative effects with IC 50 of 1-6 nM. Apoptosis AnalysisCell Line: HCC70, MDA-MB-468, CAOV3 and OVCAR3 cells Concentration: 100, 250, 500 nM Incubation Time: 48 and 72 hours Result: Induced apoptosis. Cell Cycle AnalysisCell Line: HCC70 cells Concentration: 100, 250, 500 nM Incubation Time: 48 hours Result: Induced G2/M cell cycle arrest. Western Blot AnalysisCell Line: HCC70 cells Concentration: 25, 50, 100, 250, 500 nM Incubation Time: 6, 24, 48 hours Result: Resulted in inhibition of the phosphorylation of CDK2 at Thr160 via loss of CAK function for 24 and 48 h.
In Vivo
SY-5609 (2 mg/kg/day; orally; for 21 days) induces tumor regression over the 21-day dosing period . Daily oral dosing of 2 mg/kg SY-5609 in mice provided a plasma exposure of 261.28 ng h/mL with a C max of 50.67 ng/mL (103 nM) and an elimination half-life of 3.33 h . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Six-to-eight-week-old Balb/c nude female mice with HCC70 cell line Dosage: 2 mg/kg Administration: Orally; daily; for 21 days Result: Induced tumor regression over the 21-day dosing period and was well tolerated. No regrowth of tumor was observed out to day 28.
