| Identification | Back Directory | [Name]
P276-00 (free base) | [CAS]
920113-02-6 | [Synonyms]
Riviciclib
P276-00 (free base)
Riviciclib (P276-00)
RIVICICLIB (P276-00 FREE BASE)
2-(2-chlorophenyl)-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl]chromen-4-one
2-(2-chlorophenyl)-5,7-dihydroxy-8-((2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4H-chromen-4-one
2-(2-Chlorophenyl)-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-4H-1-benzopyran-4-one
4H-1-Benzopyran-4-one, 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]- | [Molecular Formula]
C21H20ClNO5 | [MDL Number]
MFCD17215680 | [MOL File]
920113-02-6.mol | [Molecular Weight]
401.84 |
| Hazard Information | Back Directory | [Uses]
Riviciclib (P276-00 free base) is a potent cyclin-dependent kinase (CDK) inhibitor, which inhibits CDK9-cyclinT1, CDK4-cyclin D1, and CDK1-cyclinB with IC50s of 20 nM, 63 nM, and 79 nM, respectively[1][2].
Riviciclib shows antitumor activity on cisplatin-resistant cells[3]. | [in vivo]
Riviciclib (administered i.p.; 35 kg/mg daily for 10 days, in human xenograft mode with severe combined immunodeficient mice) shows significant inhibition in the growth of human colon carcinoma HCT-116 xenograft[3].
Riviciclib (administered via i.p.; 50 mg/kg once daily; 30 mg/kg twice daily for 18 treatments, in human xenograft mode with severe combined immunodeficient mice) significantly inhibits growth[3]. | Animal Model: | Human xenograft mode with HCT-116 tumor model (severe combined immunodeficient mice)[3] | | Dosage: | 35 mg/kg | | Administration: | Administered i.p.; daily for 10 days | | Result: | Given 35 mg/kg showed significant inhibition in the growth. |
| Animal Model: | Human xenograft model with H-460 tumor xenograft (severe combined immunodeficient mice)[3] | | Dosage: | 50 mg/kg; 30 mg/kg | | Administration: | Administered i.p.; 50 mg/kg once daily for 20 days; Administered i.p.; 30 mg/kg twice daily for 18 treatments | | Result: | Given 50 mg/kg and 30 mg/kg twice daily significantly inhibited growth. |
| [IC 50]
CDK9- Cyclin T1: 0.020 μM (IC50); cdk4-cyclin D1: 0.063 μM (IC50); CDK1-Cyclin B: 0.079 μM (IC50); cdk2-cyclin A: 0.224 μM (IC50); cdk2-cyclin E: 2.540 μM (IC50); cdk6-cyclin D3: 0.396 μM (IC50); CDK9-cyclin H: 2.900 μM (IC50) | [References]
[1] Roskoski R Jr,Cyclin-dependent protein kinase inhibitors including palbociclib as anticancer drugs.Pharmacol Res. 2016 May;107:249-275. DOI:10.1016/j.phrs.2016.03.012
[2] Joshi KS, et al. In vitro antitumor properties of a novel cyclin-dependent kinase inhibitor, P276-00. Mol Cancer Ther. 2007 Mar;6(3):918-25. DOI:10.1158/1535-7163.MCT-06-0613
[3] Joshi KS,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. 2007 Mar;6(3):926-34. DOI:10.1158/1535-7163.MCT-06-0614 |
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SPIRO PHARMA
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www.spiropharma.com.cn |
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InvivoChem
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BOC Sciences
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