Chemical Structure : MRT-9643
CAS No.:
3036606-92-2
MRT-9643
(MRT9643)
Catalog No.: PC-24595Not For Human Use, Lab Use Only.
MRT-9643 (MRT9643) is a potent, selective and orally active CDK2-directed molecular glue degrader, induces CDK2-dependent cancer cell growth inhibition.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
MRT-9643 (MRT9643) is a potent, selective and orally active CDK2-directed molecular glue degrader, induces CDK2-dependent cancer cell growth inhibition.
MRT-9643 engages CDK2 through a novel binding mode that does not utilize the catalytic site typically engaged by catalytic-site inhibitors, enabling superior selectivity over conserved CDKs and other kinases.
The combination of MRT-9643 and Ribociclib (CDK4/6 inhibitor) delayed resistance to CDK4/6 inhibition both in vitro and in vivo.
MRT-9643 drove deep tumor regression in combination with a CDK4/6 inhibitor or triple combination with a CDK4/6 inhibitor and endocrine therapy (fulvestrant), resulting in enhanced downstream pathway suppression as compared to a CDK4/6 inhibitor alone in preclinical models of HR-positive/HER2-negative breast cancer.
Physicochemical Properties
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M.Wt
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511.45
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Formula
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C23H22F5N5O3
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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3-(2,6-difluoro-4-((2R,3S)-2-methyl-3-((5-(3-(trifluoromethyl)bicyclo[1.1.1]pentan-1-yl)-1,3,4-oxadiazol-2-yl)amino)azetidin-1-yl)phenyl)piperidine-2,6-dione
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References
1. Patent WO2024092039 A1.
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