ChemicalBook CAS DataBase List 920113-02-6

920113-02-6

Name	P276-00 (free base)
CAS	920113-02-6
Molecular Formula	C21H20ClNO5
MDL Number	MFCD17215680
Molecular Weight	401.84
MOL File	920113-02-6.mol

Chemical Properties

Boiling point	603.3±55.0 °C(Predicted)
density	1.429±0.06 g/cm3(Predicted)
pka	6.39±0.40(Predicted)

Hazard Information

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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