SY-5609 (CDK7-IN-3) 是一种口服有效的，高选择性，非共价的 CDK7 抑制剂，K_D 为 0.065 nM。SY-5609 对 CDK2 (K_i=2600 nM)，CDK9 (K_i=960 nM)，CDK12 (K_i=870 nM) 具有较弱的抑制作用。SY-5609 诱导肿瘤细胞凋亡并具有抗肿瘤活性。

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.

Solid

CDK7 0.065 nM (Kd) CDK2 2600 nM (Ki)

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

[1]. Jason J Marineau, et al. Discovery of SY-5609: A Selective, Noncovalent Inhibitor of CDK7. J Med Chem. 2021 Nov 2.
[2]. Michael Bradley, et al. Inhibitors of cyclin-dependent kinase 7 (cdk7). WO2020093011A1.

In Vitro: DMSO : 40 mg/mL (81.56 mM; Need ultrasonic)配制储备液