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SY-5609

Catalog No. T36038 CAS 2417302-07-7

Synonyms: CDK7-IN-3

SY-5609 is a selective and noncovalent inhibitor of CDK7(KD = 0.065 nM) with antitumor activity and inhibits apoptosis.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

SY-5609, CAS 2417302-07-7

Pack Size	Availability	Price/USD
1 mg	In stock	$ 142.00
2 mg	In stock	$ 211.00
5 mg	In stock	$ 361.00
10 mg	In stock	$ 583.00
25 mg	In stock	Inquiry
50 mg	In stock	Inquiry
1 mL * 10 mM (in DMSO)	In stock	$ 419.00

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Purity: 99.34%

Purity: 99.32%

ee: 100%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SY-5609 is a selective and noncovalent inhibitor of CDK7(KD = 0.065 nM) with antitumor activity and inhibits apoptosis.
Targets&IC50	CDK12:870 nM (Ki), CDK7:0.065 nM (Kd), CDK9:960 nM (Ki), CDK2:2600 nM (Ki)
In vitro	SY-5609 (126.4 pM-4 µM) has an EC50 of 5.6 nM in the HCC70 cell line[1]. 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[2].
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[2].

Synonyms	CDK7-IN-3
Molecular Weight	490.46
Formula	C23H26F3N6OP
CAS No.	2417302-07-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 36 mg/mL (73.4 mM), Sonication is recommended.

References and Literature

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

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Bioactive Compound Library Anti-Pancreatic Cancer Compound Library Bioactive Compounds Library Max Anti-Cancer Active Compound Library Anti-Cancer Compound Library Anti-Breast Cancer Compound Library Anti-Cancer Clinical Compound Library

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Related compounds with same targets

CDK9-IN-9 CCT-251921 AG-024322 Indirubin-3′-oxime Dalpiciclib AZA197 A-443654 PHA-767491

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

SY-5609 2417302-07-7 Cell Cycle/Checkpoint CDK SY5609 SY 5609 CDK7-IN-3 inhibitor inhibit

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