P276
- Product Name
- P276
- CAS No.
- 920113-03-7
- Chemical Name
- P276
- Synonyms
- P276;CS-996;P276 USP/EP/BP;Riviciclib HCl;Riviciclib HCl (P276-00);Riviciclib hydrochloride;RIVICICLIB HYDROCHLORIDE (P276-00);Riviciclib hydrochloride, 10 mM in DMSO;inhibit,Inhibitor,Riviciclib,CDK,Riviciclib hydrochloride,Cyclin dependent kinase,Apoptosis;2-(2-Chlorophenyl)-5,7-dihydroxy-8-((2R,3S)-2-(hydroxymethyl)-1-methylpyrrolidin-3-yl)-4H-chromen-4-one HCl
- CBNumber
- CB32668296
- Molecular Formula
- C21H21Cl2NO5
- Formula Weight
- 438.3
- MOL File
- 920113-03-7.mol
P276 Property
- storage temp.
- Store at -20° C
- solubility
- Soluble in DMSO
- form
- Solid
- color
- Off-white to light yellow
N-Bromosuccinimide Price
- Product number
- CS-0006648
- Product name
- Riviciclibhydrochloride
- Purity
- 98.33%
- Packaging
- 5mg
- Price
- $180
- Updated
- 2021/12/16
- Product number
- CS-0006648
- Product name
- Riviciclibhydrochloride
- Purity
- 98.33%
- Packaging
- 10mg
- Price
- $300
- Updated
- 2021/12/16
- Product number
- 60932
- Product name
- P276-00
- Packaging
- 1mg
- Price
- $650
- Updated
- 2021/12/16
- Product number
- CD11014532
- Product name
- P276-00(RivicilibHydrocloride)
- Purity
- 95+%
- Packaging
- 5mg
- Price
- $107
- Updated
- 2021/12/16
- Product number
- CD11014532
- Product name
- P276-00(RivicilibHydrocloride)
- Purity
- 95+%
- Packaging
- 10mg
- Price
- $179
- Updated
- 2021/12/16
P276 Chemical Properties,Usage,Production
Uses
P276-00 is a cyclin-dependent kinase (CDK) inhibitor. P276-00 has shown to be highly selective for cancer cells and has shown to produce potent inhibition of Cdk4-D1 activity. P276-00 also induces apoptosis in human promyelocytic leukemia (HL-60) cells.
Enzyme inhibitor
This cell cycle-inhibiting flavone and anticancer agent (FW = 438.30 g/mol; CAS 920113-03-7), also named 2-(2-chlorophenyl)-5,7-dihydroxy-8- [(2R,3S)-2-(hydroxymethyl)-1-methyl-3-pyrrolidinyl]-4H-1-benzopyran-4- one, targets the Cyclin-Dependent Kinases CDK1 (IC50 = 79 nM), CDK4 (IC50 = 63 nM) and CDK9 (IC50 = 20 nM). p276-00 showed potent antiproliferative effects against various human cancer cell lines (IC50 values ranging from 300 to 800 nmol/L), but has little effect on cultured fibroblasts. A significant down-regulation of cyclin D1 and Cdk4 and a decrease in Cdk4-specific pRb Ser(780) phosphorylation is observed. P276-00 produces potent inhibition of Cdk4-D1 activity that is competitive with ATP, and not with retinoblastoma protein. The compound also induced apoptosis in human promyelocytic leukemia (HL-60) cells, as evidenced by the induction of caspase-3 and DNA ladder studies. In 22 human cancer xenografts, P276-00 is approximately 26x more potent than cisplatin, and is also active against cisplatin-resistant tumors of central nervous system, melanoma, prostate, and renal cancers. Synchronized human non-small cell lung carcinoma (H-460) and human normal lung fibroblast (WI-38) cells are arrested in G1
in vivo
Riviciclib hydrochloride (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 hydrochloride (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 inhibited 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: 2.500 μM (IC50); cdk6-cyclin D3: 0.396 μM (IC50); CDK9-cyclin H: 2.900 μM (IC50)
P276 Preparation Products And Raw materials
Raw materials
Preparation Products
P276 Suppliers
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