146426-40-6
Flavopiridol
CAS: 146426-40-6
Molecular Formula: C21H20ClNO5
146426-40-6 - Names and Identifiers
| Name | Flavopiridol |
| Synonyms | C077990 L 868275 Hmr 1275 Alvocidib Flavopirodol FLAVOPIRIDOL Flavopiridol 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3s,4r)-3-hydroxy-1-methyl-4-piperidyl]chromen-4-one 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3R,4S)-3-hydroxy-1-methylpiperidin-4-yl]-4H-chromen-4-one (-)cis-5,7-Dihydroxy-2-(2-chlorophenyl)-8-(4-(3-hydroxy-1-methyl)piperidinyl)-4H-1-benzopyran-4-one 4H-1-Benzopyran-4-one, 2-(2-chlorophenyl)-5,7-dihydroxy-8-[(3S,4R)-3-hydroxy-1-methyl-4-piperidinyl]- |
| CAS | 146426-40-6 |
| InChI | InChI=1/C21H20ClNO5/c1-23-7-6-12(17(27)10-23)19-14(24)8-15(25)20-16(26)9-18(28-21(19)20)11-4-2-3-5-13(11)22/h2-5,8-9,12,17,24,26-27H,6-7,10H2,1H3/t12-,17+/m1/s1 |
146426-40-6 - Physico-chemical Properties
| Molecular Formula | C21H20ClNO5 |
| Molar Mass | 401.84 |
| Density | 1.448±0.06 g/cm3(Predicted) |
| Melting Point | 52.5 °C |
| Boling Point | 603.6±55.0 °C(Predicted) |
| Solubility | DMSO : 33.33 mg/mL (82.94 mM; Need ultrasonic) |
| Appearance | Light yellow to yellow (Solid) |
| pKa | 6.16±0.40(Predicted) |
| Storage Condition | 2-8°C |
| Refractive Index | 1.708 |
| MDL | MFCD20501884 |
| In vitro study | As a broad-spectrum inhibitor of CDK, Flavopiridol can inhibit cell cycle progression and stop it at G1 or G2 phase. 0.3 μm Flavopiridol acts on MCF-7 or MDA-MB-468 cells and induces cell cycle arrest at G1 phase by inhibiting CDK4 or CDK2 kinase activity. Flavopiridol acts on unrelated kinases, such as MAP, PAK, PKC, and EGFR, with much lower activity, IC50 >14 μm. Flavopiridol significantly inhibited the growth of HCT116, A2780, PC3, and Mia PaCa-2 colonies with IC50 of 13 nM, 15 nM, 10 nM, and 36 nM, respectively. Flavopiridol acts on a variety of tumor cell lines and is cytotoxic. The IC50 ranges from 16 nM for LNCAP to 130 nM for K562. Flavopiridol also potently inhibits glycogen synthase kinase -3(GSK-3) activity with an IC50 of 280 nm. Compared with other CDKs, Flavopiridol was slightly less effective in inhibiting CDK7 activity, with an IC50 of 875 nM. Flavopiridol (0.5 μM) pSer807/811 Rb and pThr199 NPM were inhibited, while slight changes were observed on pThr821 Rb. Flavopiridol also reduces the level of all RNA polymerase II, and RNA polymerase II is phosphorylated at the Ser2 Ser5 site in the CTD repeat. |
| In vivo study | Treatment of P388 mouse leukemia with Flavopiridol at a dose of 7.5 mg/kg for 7 days had slight anticancer activity resulting in a% T/C value of 110, and effective in the subcutaneous inhibition of human A2780 ovarian cancer in nude mice, the cell log kill (LCK) is 1.5. Flavopiridol at a dose of 1-2.5 mg/kg for 10 days significantly inhibited collagen-induced arthritis by inhibiting synovial hyperplasia and joint damage in a dose-dependent manner, however, serum concentrations of anti-type II collagen (CII) antibodies, and proliferation corresponding to type II collagen, remained unchanged. |
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Spot supply
Product Name: Alvocidib Visit Supplier Webpage Request for quotationCAS: 146426-40-6
Tel: 0714-3999186
Email: 2853786052@qq.com
Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Multiple SpecificationsSpot supply
Product Name: Alvocidib Visit Supplier Webpage Request for quotationCAS: 146426-40-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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