[CAS NO. 920113-03-7] Riviciclib hydrochloride (P276-00)

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PRODUCTS SPECIFICATIONS [920113-03-7]

Catalog

SLK-S8058

Brand

Selleck

CAS

920113-03-7

DESCRIPTION [920113-03-7]

Overview

MDL	-
Molecular Weight	438.3
Molecular Formula	C21H20ClNO5.HCl
SMILES	OC=1C(=C2C(C(=O)C=C(O2)C3=C(Cl)C=CC=C3)=C(O)C1)[C@H]4[C@H](CO)N(C)CC4.Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Description

Riviciclib hydrochloride (P276-00) is a novel , and inhibitor with of 79 nM, 63 nM and 20 nM, respectively. Riviciclib hydrochloride (P276-00) induces apoptosis. Phase 2/3.

Targets

In vitro

P276-00 shows 40-fold selectivity toward Cdk4-D1, compared with Cdk2-E. It shows potent antiproliferative effects against various human cancer cell lines, including HCT-116, U2OS, H-460, HL-60, HT-29, SiHa, MCF-7, Colo-205, SW-480, PC-3, Caco2, T-24 with an IC50 ranging from 300 to 800 nmol/L, and is found to be highly selective for cancer cells as compared with normal fibroblast cells. P276-00 can down-regulate cyclin D1 and Cdk4 in an ATP- competitive manner and decrease Cdk4-specific pRb Ser780 phosphorylation. P276-00 also induces apoptosis by actving cellular caspase-3 activity and DNA ladder formation.

In vivo

P276-00, administered i.p. at 50 mg/kg daily for 20 treatments can significantly induce growth inhibition of murine colon cancer (CA-51). However, in murine lung carcinoma model (Lewis lung), an increased dose of 60 mg/kg (30 mg/kg twice daily) administered every alternate day i.p. for 7 treatments shows significant inhibition in the growth. And it also inhibit the growth of human colon carcinoma HCT-116 xenograft and human non-small cell lung carcinoma H-460 xenograft. Efficacy Studies show its maximum tolerated dose is 78 mg/kg/d.

References

[1] Joshi KS, et al. Mol Cancer Ther, 2007, 6(3), 918-925.
[2] Joshi KS, et al. Mol Cancer Ther, 2007, 6(3), 926-934.

Synonyms

4H-1-Benzopyran-4-one, 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-, hydrochloride (1:1)

P 276-00