Fadraciclib (CYC065)

Catalog No.S7371

For research use only.

Fadraciclib (CYC065) is a novel, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50 of 5 nM and 26 nM, respectively.

Fadraciclib (CYC065) Chemical Structure

CAS No. 1070790-89-4

Purity & Quality Control

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Biological Activity

Description Fadraciclib (CYC065) is a novel, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50 of 5 nM and 26 nM, respectively.
Targets
CDK2 [1]
()
CDK9 [1]
()
5 nM 26 nM
In vitro

Fadraciclib effectively downregulates pro-survival and leukemogenic proteins and that short pulse treatment is sufficient to substantially decrease cell viability of the majority of AML cell lines tested via apoptotic induction.<sup><a class="sref" href="#s_ref">[1]</a></sup>

In vivo

Fadraciclib shows potent anti-leukemic activity in two subcutaneous xenograft models EOL-1 (with MLL-PTD) and HL60 (non MLLr/MLL-PTD AML with MYC amplification).<sup><a class="sref" href="#s_ref">[1]</a></sup>

Protocol (from reference)

Cell Research:

<sup><a class="sref" href="#s_ref">[2]</a></sup>

  • Cell lines: AML cell lines
  • Concentrations: 1 μM
  • Incubation Time: 72 h
  • Method:

    Half-maximal inhibitory concentration (IC50) of AML cell lines treated with fadraciclib for up to 72 h was established using 7-Hydroxy-3H-phenoxazin-3-one-10-oxide sodium salt resazurin assay according to manufacturer’s instructions. IC50 were calculated using GraphPad Prism 8 software (GraphPad Software).

Animal Research:

<sup><a class="sref" href="#s_ref">[1]</a></sup>

  • Animal Models: Female athymic CB-17 SCID (Harlan Sprague-Dawley) mice
  • Dosages: 40 or 55 mg/kg
  • Administration: Oral gavage

Solubility (25°C)

In vitro

DMSO 80 mg/mL
(201.24 mM)
Water Insoluble
Ethanol ''80 mg/mL

Chemical Information

Molecular Weight 397.52
Formula

C21H31N7O

CAS No. 1070790-89-4
Storage 3 years -20°C powder
2 years -80°C in solvent

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02552953 Unknown status Drug: CYC065 Cancer Cyclacel Pharmaceuticals Inc. September 2015 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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