A pan-CDK inhibitor
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Voruciclib

Item No. 29085

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[2-chloro-4-(trifluoromethyl)phenyl]-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-4H-1-benzopyran-4-one
CAS Number
1000023-04-0
Molecular Formula
C22H19ClF3NO5
Formula Weight
469.8
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
269 nm
SMILES
O=C1C=C(C2=C(Cl)C=C(C(F)(F)F)C=C2)OC3=C1C(O)=CC(O)=C3[C@@]4([H])[C@H](CO)N(C)CC4
InChi Code
InChI=1S/C22H19ClF3NO5/c1-27-5-4-12(14(27)9-28)19-15(29)7-16(30)20-17(31)8-18(32-21(19)20)11-3-2-10(6-13(11)23)22(24,25)26/h2-3,6-8,12,14,28-30H,4-5,9H2,1H3/t12-,14+/m1/s1
InChi Key
MRPGRAKIAJJGMM-OCCSQVGLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Voruciclib is a pan-inhibitor of cyclin-dependent kinases (CDKs; Kis = 0.626-9.1 nM).1 It is selective for CDKs over male germ cell associated kinase (MAK) and intestinal cell kinase (ICK; Kis = 259 and 481 nM, respectively), in a panel of 48 kinases. Voruciclib decreases myeloid cell leukemia-1 (Mcl-1) levels and increases cleaved poly(ADP-ribose) polymerase (PARP) levels in six diffuse large B-cell lymphoma (DLBCL) cell lines when used at concentrations ranging from 0.5 to 5 µM. It reduces tumor growth by 56.3% in a Ri-1 mouse xenograft model when administered at a dose of 200 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dey, J., Deckwerth, T.L., Kerwin, W.S., et al. Voruciclib, a clinical stage oral CDK9 inhibitor, represses MCL-1 and sensitizes high-risk diffuse large B-cell lymphoma to BCL2 inhibition. Sci. Rep. 7(1), 18007 (2017).