SY-5609

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CDK7-IN-3 是一种选择性 CDK7 抑制剂，KD 为 0.059 nM。 CDK7-IN-3 对 CDK2 (Ki=390 nM)、CDK9 (Ki=290 nM)、CDK12 (Ki=78 nM) 的抑制作用较差。 CDK7-IN-3 诱导肿瘤细胞凋亡并具有抗肿瘤活性。

CDK7-IN-3 is a selective CDK7 inhibitor with a KD of 0.059 nM. CDK7-IN-3 shows poor inhibition on CDK2 (Ki=390 nM), CDK9 (Ki=290 nM), CDK12 (Ki=78 nM). CDK7-IN-3 induce apoptosis in tumor cells and has antitumor activity.(In Vitro):SY-5609 (126.4 pM-4 μM) has an EC50 of 5.6 nM in the HCC70 cell line. SY-5609 (0.01-10000 nM) exhibits strong antiproliferative effects with IC50s of 1-6 nM in triple-negative breast cancer and ovarian cancer cells including HCC70, MDA-MB453, COV504, A2780, OVCAR3, CAOV3 cells. SY-5609 (100-500 nM) induces apoptosis in HCC70, MDA-MB-468, CAOV3, and OVCAR3 cells. In HCC70 cells, SY-5609 (100-500 nM) induces G2/M cell cycle arrest. SY-5609 (25-500 nM) inhibits the phosphorylation of CDK2 at Thr160 via loss of CAK function.(In Vivo):In Balb/c nude female mice with HCC70 cell lines, SY-5609 (2 mg/kg/day; orally) induces tumor regression with a plasma exposure of 261.28 ng h/mL, a Cmax of 50.67 ng/mL and an elimination half-life of 3.33 h.

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 EC50 of 5.6 nM in HCC70 cell line.Cell Proliferation Assay Cell Line:HCC70, MDA-MB453, COV504, A2780, OVCAR3, CAOV3 cells Concentration:0.01-10000 nM Incubation Time:72 hours Result:Demonstrated strong antiproliferative effects with IC50 of 1-6 nM.Apoptosis Analysis Cell 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 Analysis Cell Line:HCC70 cells Concentration:100, 250, 500 nM Incubation Time:48 hours Result:Induced G2/M cell cycle arrest.Western Blot Analysis Cell 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.

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 Cmax of 50.67 ng/mL (103 nM) and an elimination half-life of 3.33 h. 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.

CDK7-IN-3

Others

Other Targets

Adenosine receptor

——

——

2417302-07-7

490.46

C23H26F3N6OP

>98% (HPLC)

In Vitro:?DMSO : 40 mg/mL (81.56 mM)

N/A

——

(-20℃)

With Ice Pack

≥ 2 years