A Cdk9, Cdk4, and Cdk1 inhibitor
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P276-00 (hydrochloride)

Item No. 39845

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-4H-1-benzopyran-4-one, monohydrochloride
CAS Number
920113-03-7
Synonyms
  • Riviciclib
Molecular Formula
C21H20ClNO5 • HCl
Formula Weight
438.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: SolubleDMSO: Soluble
SMILES
OC1=CC(O)=C(C(C=C(C2=CC=CC=C2Cl)O3)=O)C3=C1[C@@H]4CCN([C@H]4CO)C.Cl
InChi Code
InChI=1S/C21H20ClNO5.ClH/c1-23-7-6-12(14(23)10-24)19-15(25)8-16(26)20-17(27)9-18(28-21(19)20)11-4-2-3-5-13(11)22;/h2-5,8-9,12,14,24-26H,6-7,10H2,1H3;1H/t12-,14+;/m1./s1
InChi Key
OOVTUOCTLAERQD-OJMBIDBESA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $98

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    5 mg

    $294

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    10 mg

    $539

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    Product Description

    P276-00 is an inhibitor of cyclin-dependent kinase 9 (Cdk9), Cdk4, and Cdk1 (IC50s = 0.020, 0.063, and 0.079 µM, respectively).1 It is selective for these CDKs over Cdk2/cyclin E, Cdk2/cyclin A, Cdk6, and Cdk7 (IC50s = 2.54, 0.224, 0.396, and 2.87 µM, respectively), as well as a panel of eight other kinases. P276-00 (1 µM) induces apoptosis in HL-60 leukemia cells. It induces cell cycle arrest at the G1 phase in synchronized H460 non-small cell lung cancer (NSCLC) cells when used at concentrations of 1.5 and 5 µM.2 P276-00 (50 mg/kg once per day) reduces tumor volume in an H460 mouse xenograft model. It also inhibits reactivation of latent HIV-1 induced by the HIV re-activator prostratin (Item No. 10272), pan-HDAC inhibitor panobinostat (Item No. 13280), or bromodomain inhibitor JQ-1 in 24ST1NLESG cells (IC50s = 0.1, 0.07, and 0.075 µM, respectively).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Joshi, K.S., Rathos, M.J., Joshi, R.D., et al. In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00. Mol. Cancer Ther. 6(3), 918-925 (2007).

    2. Joshi, K.S., Rathos, M.J., Mahajan, P., et al. P276-00, a novel cyclin-dependent inhibitor induces G1-G2 arrest, shows antitumor activity on cisplatin-resistant cells and significant in vivo efficacy in tumor models. Mol. Cancer Ther. 6(3), 926-934 (2007).

    3. Vargas, B., Giacobbi, N.S., Sanyal, A., et al. Inhibitors of signaling pathways that block reversal of HIV-1 latency. Antimicrob. Agents Chemother. 63(2), e01744-01718 (2019).