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Datasheet of LDC-4297

Description:.
In vitro: LDC4297 inhibits CDK7 in vitro in the nano-picomolar range. The affinity of LDC4297 for CDK7 proves to be
extremely high. The replication of HCMV in cultured primary human fibroblasts (HFFs) is inhibited by LDC4297 in a
concentration-dependent manner with a 50% effective concentration (EC50) value of 24.5 1.3 nM. Notably, CDK7 inhibition
by LDC4297 is not associated with general cytotoxicity at submicromolar concentrations. In contrast, LDC4297 induces
cytotoxicity in a set of tumor cell lines, i.e., already at extremely low, nanomolar concentrations in specific cases. Anti-HCMV
activity of LDC4297 is exerted through a multifaceted mode of action that involves an interference with virus-induced Rb
phosphorylation. In vivo: The PK analyses of LDC4297 performed thus far have also been highly promising. An analysis of the
PK parameters in CD1 mice reveals positive characteristics after oral administration, as demonstrated for a single-dose treatment
(100 mg/kg of LDC4297. The half-life (t1/2z) is determined to be 1.6 h, and a time (Tmax) to a mean peak plasma concentration
of 1,297.6 ng/ml is reached 0.5 h after administration, with a continued presence of LDC4297 plasma levels for at least 8 h and a
bioavailability of 97.7%.

Chemical Information

Catalog DC10143

Purity of current batch: >98%

Molecular Weight (MW) 432.52

Molecular Formula C23H28N8O

CAS No. 1453834-21-3

Solubility (25C) DMSO

Storage Store at -20C (desiccating conditions).

Handling:
Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months.
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in
advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20C. Generally, these will be useable
for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room
temperature for at least 1 hour.