Home Cell Cycle CDK inhibitor Fadraciclib (CYC065) For research use only.

Fadraciclib (CYC065)

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

Fadraciclib (CYC065) Chemical Structure

CAS No. 1070790-89-4

Purity & Quality Control

Batch: S737101 DMSO]80 mg/mL]false]Ethanol]80 mg/mL]false]Water]Insoluble]false Purity: 99.88%
99.88

Fadraciclib (CYC065) Related Products

Signaling Pathway

CDK Signaling Pathways

CDK Signaling Pathway

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
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>
Cell Research 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).
In Vivo
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>
Animal Research Animal Models Female athymic CB-17 SCID (Harlan Sprague-Dawley) mice
Dosages 40 or 55 mg/kg
Administration Oral gavage
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05817890 Active not recruiting
Healthy
Cyclacel Pharmaceuticals Inc.
 March 3 2023 Early Phase 1
NCT02552953 Completed
Cancer
Cyclacel Pharmaceuticals Inc.
 September 28 2015 Phase 1

Chemical Information & Solubility

Molecular Weight 397.52 Formula

C21H31N7O
CAS No. 1070790-89-4 SDF --
Smiles CCC(NC1=NC(=C2N=C[N](C(C)C)C2=N1)NCC3=C(C)C=C(C)N=C3)C(C)O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 80 mg/mL ( (201.24 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 80 mg/mL

Water : Insoluble


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In vivo
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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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