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Fadraciclib (CYC065) CDK inhibitor

Cat.No.S7371

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

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

Solubility

In vitro
Batch:

DMSO : 80 mg/mL (201.24 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 80 mg/mL

Water : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 397.52 Formula

C21H31N7O

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1070790-89-4 -- Storage of Stock Solutions

Synonyms N/A SMILES CCC(NC1=NC(=C2N=C[N](C(C)C)C2=N1)NCC3=C(C)C=C(C)N=C3)C(C)O

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Mechanism of Action

Targets/IC50/Ki
CDK2
5 nM
CDK9
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>

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-10)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02813135 RECRUITING
Pediatric Cancer
Gustave Roussy, Cancer Campus, Grand Paris
2016-08-03 PHASE1; PHASE2
NCT04983810 UNKNOWN
Solid Tumor, Adult; Lymphoma
Cyclacel Pharmaceuticals, Inc.
2021-07-12 PHASE1; PHASE2
NCT05168904 SUSPENDED
Leukemia; Myelodysplastic Syndrome(MDS)
Cyclacel Pharmaceuticals, Inc.
2021-10-22 PHASE1; PHASE2
NCT05817890 COMPLETED
Healthy
Cyclacel Pharmaceuticals, Inc.
2023-03-03 EARLY_PHASE1
NCT05817890 Active not recruiting
Healthy
Cyclacel Pharmaceuticals Inc.
2023-03-03 Early Phase 1
NCT04017546 COMPLETED
AML; MDS
Cyclacel Pharmaceuticals, Inc.
2019-08-02 PHASE1

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