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SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a KD of 0.065 nM. SY-5609 shows poor inhibition on CDK2 (Ki=2600 nM), CDK9 (Ki=960 nM), CDK12 (Ki=870 nM). SY-5609 induces apoptosis in tumor cells and has antitumor activity.
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 (126.4 pM-4 µM; 72 hours) has an EC50 of 5.6 nM in HCC70 cell line.
In vivo, SY-5609 (2 mg/kg/day; orally; for 21 days) induces tumor regression over the 21-day dosing period.
| Molecular Weight | 490.46 |
| Formula | C23H26F3N6OP |
| CAS Number | 2417302-07-7 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage | 4°C, sealed |
[3] Georgina P Sava, et al. Cancer Metastasis Rev. CDK7 inhibitors as anticancer drugs
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