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2052301-24-1

2052301-24-1 Structure

2052301-24-1 Structure
IdentificationBack Directory
[Name]

BTX161
[CAS]

2052301-24-1
[Synonyms]

BTX161
[Molecular Formula]

C15H16N2O3
[MDL Number]

MFCD34578207
[MOL File]

2052301-24-1.mol
[Molecular Weight]

272.3
Chemical PropertiesBack Directory
[Boiling point ]

558.7±50.0 °C(Predicted)
[density ]

1.301±0.06 g/cm3(Predicted)
[storage temp. ]

Store at -20°C
[form ]

Solid
[pka]

10.83±0.40(Predicted)
[color ]

White to off-white
Hazard InformationBack Directory
[Biological Activity]

BTX161, a Thalidomide analog, is a potent CKIα degrader. BTX161 mediates degradation of CKIα better than Lenalidomide in human AML cells and activates DNA damage response (DDR) and p53, while stabilizing the p53 antagonist MDM2[1]. BTX161 (25 μM; 4 hours; MV4-11 cells) upregulates all the Wnt targets including MYC and did not affect MDM2 mRNA expression[1].BTX161 (10 μM; 6 hours; MV4-11 cells), on its own, augmented p53 and MDM2 protein expression, yet in combination with THZ1, and particularly with both THZ1 and CDK9, further augmented p53 and induced maximal caspase 3 activation[1].
[References]

[1]. Minzel W, et al. Small Molecules Co-targeting CKIα and the Transcriptional Kinases CDK7/9 Control AML in Preclinical Models. Cell. 2018;175(1):171-185.e25.
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