| Bioactivity | 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[1][2]. |
| Invitro | SY-5609 (0.01-10000 nM; 72 hours) demonstrates strong antiproliferative effects in triple negative breast cancer (TNBC) and ovarian (OVA) cancer cells[1]. SY-5609 (100-500 nM; 48, 72 hours) induces apoptosis[1]. SY-5609 (100-500 nM; 48 hours) induces G2/M cell cycle arrest in HCC70 cells[1]. 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[1]. SY-5609 (compound 101; 126.4 pM-4 µM; 72 hours) has an EC50 of 5.6 nM in HCC70 cell line[2]. Cell Proliferation Assay[1] Cell Line: |
| Name | SY-5609 |
| CAS | 2417302-07-7 |
| Formula | C23H26F3N6OP |
| Molar Mass | 490.46 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
SY-5609
CAS: 2417302-07-7 F: C23H26F3N6OP W: 490.46
SY-5609 (CDK7-IN-3) is an orally active, highly selective, noncovalent CDK7 inhibitor with a KD of 0.065 nM. SY-5609 sho
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