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SY-5102

Chemical Structure : SY-5102

CAS No.: 2365230-48-2

SY-5102 (SY5102)

Catalog No.: PC-72466Not For Human Use, Lab Use Only.

SY-5102 (SY5102) is a highly potent, selective, noncovalent, orally available CDK7 inhibitor with SPR Kd of 0.03 nM (binding to CDK7/Cyclin H).

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

SY-5102 (SY5102) is a highly potent, selective, noncovalent, orally available CDK7 inhibitor with SPR Kd of 0.03 nM (binding to CDK7/Cyclin H).
SY-5102 (SY5102) displays highly selectivity against CDK2, CDK9, and CDK12 (all IC50>75 nM).
SY-5102 potently inhibits HCC70 cell proliferation with EC50 of 9 nM.
SY-5102 showed dose-dependent tumor growth inhibition including tumor regression at 4 mg/kg po (dosed twice daily) in an HCC70 cell line derived xenograft mouse model.

Physicochemical Properties

M.Wt 457.45
Formula C22H22F3N7O
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Month
Shipping
Solubility

Chemical Name/SMILES

References

1. Jason J Marineau, et al. J Med Chem. 2022 Jan 27;65(2):1458-1480.

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