An inhibitor of Cdk2 and Cdk9
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Fadraciclib

Item No. 36119

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2R,3S)-3-[[6-[[(4,6-dimethyl-3-pyridinyl)methyl]amino]-9-(1-methylethyl)-9H-purin-2-yl]amino]-2-pentanol
CAS Number
1070790-89-4
Synonyms
  • CYC065
Molecular Formula
C21H31N7O
Formula Weight
397.5
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
213, 231 nm
SMILES
CC[C@H](NC1=NC(NCC2=CN=C(C=C2C)C)=C3N=CN(C(C)C)C3=N1)[C@@H](C)O
InChi Code
InChI=1S/C21H31N7O/c1-7-17(15(6)29)25-21-26-19(18-20(27-21)28(11-24-18)12(2)3)23-10-16-9-22-14(5)8-13(16)4/h8-9,11-12,15,17,29H,7,10H2,1-6H3,(H2,23,25,26,27)/t15-,17+/m1/s1
InChi Key
DLPIYBKBHMZCJI-WBVHZDCISA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $57

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    5 mg

    $266

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    10 mg

    $475

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    25 mg

    $1,043

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    Product Description

    Fadraciclib is an inhibitor of cyclin-dependent kinase 2 (Cdk2) and Cdk9 (IC50s = 4.5 and 20.5 nM, respectively).1 It is selective for Cdk2 and Cdk9 over Cdk1, -4, and -7 (IC50s = 278, 193, and 232 nM, respectively). Fadraciclib inhibits the proliferation of COLO 205 cells (IC50 = 0.31 µM), as well as inhibits proliferation in a panel of five breast cancer cell lines (IC50s = <0.4 µM for all). It decreases phosphorylation of the RNA polymerase II C-terminal domain and RB, Cdk9 and Cdk2 targets, respectively, and induces apoptosis in COLO 205 cells. Fadraciclib (40 and 55 mg/kg) reduces tumor volume in an EoL-1 eosinophilic leukemia mouse xenograft model. It also inhibits tumor growth in an HL-60 mouse xenograft model when administered at a dose of 70 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Frame, S., Saladino, C., MacKay, C., et al. Fadraciclib (CYC065), a novel CDK inhibitor, targets key pro-survival and oncogenic pathways in cancer. PLoS One 15(7), e0234103 (2020).