3106928-52-0
Chemical Structure
AMC-3-221
- CAS No.: 3106928-52-0
- Formula:C35H34Cl2FN9O7
- Molecular Weight:782.60
InChIKey: IZSBMEKHWRDITN-UHFFFAOYSA-N
SMILES: FC1=CC2=C(C(N(C3C(NC(CC3)=O)=O)C2=O)=O)C=C1N(CC4)CCN4C(CN5CCC(NC(C6=NNC=C6NC(C7=C(Cl)C=CC=C7Cl)=O)=O)CC5)=O
Biological Activity: AMC-3-221 is a cereblon-dependent CDK9 PROTAC degrader with a DC50 of 8 nM (MOLM14 AML cells). AMC-3-221 targets CDK9 with an IC50 of 1.7 nM and a Kd of 4.6 nM. AMC-3-221 decreases MCL-1 and c-MYC protein levels as well as MCL-1, c-MYC, and N-MYC RNA levels. AMC-3-221 induces apoptosis and inhibits proliferation in multiple cancer cell lines. AMC-3-221 exhibits proteasome-dependent CDK9 degradation. AMC-3-221 can be used for research on acute myeloid leukemia (AML)[1].
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AMC-3-221 | AMC-3-221 is a cereblon-dependent CDK9 PROTAC degrader with a DC50 of 8 nM (MOLM14 AML cells). AMC-3-221 targets CDK9 with an IC50 of 1.7 nM and a Kd of 4.6 nM. AMC-3-221 decreases MCL-1 and c-MYC protein levels as well as MCL-1, c-MYC, and N-MYC RNA levels. AMC-3-221 induces apoptosis and inhibits proliferation in multiple cancer cell lines. AMC-3-221 exhibits proteasome-dependent CDK9 degradation. AMC-3-221 can be used for research on acute myeloid leukemia (AML). | |||||||||||||||||||||
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