Alvocidib - CAS 146426-40-6
Not Intended for Therapeutic Use. For research use only.
Category:
Inhibitor
Product Name:
Alvocidib
Catalog Number:
146426-40-6
Synonyms:
Flavopiridol; HMR 1275.
CAS Number:
146426-40-6
Description:
Alvocidib is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis.
COA:
Inquire
MSDS:
Inquire
Targets:
CDK
Current Developer:
Sanofi-Aventis Inc.
Chemical Structure
CAS 146426-40-6 Alvocidib

Related CDK Products


KH-CB19
(CAS: 1354037-26-5)

KH-CB19, a CLK1/CLK4 inhibitor, has been found to probably restrain the phosphorylation of serine- and arginine-rich (SR) proteins. IC50: 20 nM for CLK1.

CAS 779353-01-4 Dinaciclib

Dinaciclib
(CAS: 779353-01-4)

Dinaciclib, also known as SCH727965, is a potent CDK inhibitor with potential antineoplastic activity. Dinaciclib selectively inhibits cyclin dependent kinases ...

CAS 377090-84-1 SU9516

SU9516
(CAS: 377090-84-1)

SU 9516 is a potent, selective cdk2 inhibitor (IC50 values are 0.022, 0.04, >10, >10, 18 and >100 μM for cdk2, cdk1, cdk4, PKC, p38, PDGFR and EGFR respectively...

CAS 345627-80-7 SNS-032

SNS-032
(CAS: 345627-80-7)

SNS-032, also known as BMS-387032, is a 2-aminothiazole-derived, small-molecule cyclin dependent kinase (CDK) inhibitor with potential antineoplastic activity. ...

CAS 146426-40-6 Alvocidib

Alvocidib
(CAS: 146426-40-6)

Alvocidib is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by p...

CAS 212779-48-1 NG 52

NG 52
(CAS: 212779-48-1)

NG 52 is a tri-substituted purine that binds to the ATP-binding site of yeast cyclin-dependent kinases, inhibiting Cdc28p and Pho85p (IC50s = 7 and 2 µM, respec...

CAS 1231930-82-7 LY2835219

LY2835219
(CAS: 1231930-82-7)

LY2835219 is a potent and selective inhibitor of CDK4 and CDK6 with IC50 of 2 nM and 10 nM, respectively. Phase 3.

CAS 784210-87-3 RGB-286638

RGB-286638
(CAS: 784210-87-3)

RGB-286638 is a novel CDK inhibitor. It inhibited several tyrosine and serine/threonine non-CDK enzymes, i.e. GSK-3β, TAK1, AMPK, Jak2, MEK1. It demonstrated eq...

CAS 718630-59-2 PHA-793887

PHA-793887
(CAS: 718630-59-2)

PHA-793887 is an inhibitor of multiple cyclin dependent kinases (CDK) with activity against CDK2, CDK1 and CDK4. Although toxicity was acceptable at initial dos...

CAS 741713-40-6 R547

R547
(CAS: 741713-40-6)

R547 is orally bioavailable diaminopyrimidine cyclin-dependent kinase inhibitor (CDKI) with potential antineoplastic activity. CDKI R547 selectively binds to an...

CAS 845714-00-3 PHA-767491

PHA-767491
(CAS: 845714-00-3)

PHA-767491 is a potent, ATP-competitive dual cdc7/cdk9 inhibitor (IC50 values are 10 and 34 nM respectively) that prevents initiation of DNA replication.

CAS 1211441-98-3 Ribociclib

Ribociclib
(CAS: 1211441-98-3)

Ribociclib, also known as LEE011, is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway,...

Ca2+ Channel Agonist 1
(CAS: 1402821-24-2)

A Ca2+ Channel Agonist that selectively acting on N-type Ca2+ channel and also be found to restrain the cdk activity at some extent. IC50: 14.23 uM (EC50, Ca2+ ...

CAS 1431697-85-6 AT7519 trifluoroacetate

AT7519 trifluoroacetate
(CAS: 1431697-85-6)

AT7519 is an ATP competitive CDK inhibitor with a Ki value of 38 nM for CDK1. AT7519 is inactive against all non-CDK kinases with the exception of GSK3β (IC50 =...

THZ1-R
(CAS: 1621523-07-6)

THZ1-R, with the potential to treat Triple-negative breast cancer (TNBC), it is a potent and selective CDK7 inhibitor but has instability in vivo.

CAS 212844-53-6 Purvalanol A

Purvalanol A
(CAS: 212844-53-6)

Purvalanol A is a potent CDK inhibitor, which effectively suppresses Src-mediated transformation by inhibiting both CDKs and c-Src. indicating that the activati...

CAS 1421693-22-2 CDKI-73

CDKI-73
(CAS: 1421693-22-2)

CDKI-73 was cytotoxic to all of the CLL samples tested (n = 38) with a mean LD50 value of 0.08μM ± 0.10 μM following exposure to drug for 48h. In contrast, norm...

CAS 153437-55-9 WHI-P180 hydrochloride

WHI-P180 hydrochloride
(CAS: 153437-55-9)

WHI-P180 moderately inhibited ABCG2 function, exhibiting weak phototoxicity. The elimination half-life of WHI-P180 in CD-1 mice (BALB/ c mice) following i.v., i...

THZ2
(CAS: 1604810-84-5)

THZ2, an analog of THZ1, with the potential to treat Triple-negative breast cancer (TNBC), it is a potent and selective CDK7 inhibitor which overcomes the insta...

ON123300
(CAS: 1357470-29-1)

ON123300, a dihydropyrido[2,3-d]pyrimidine derivative, has been found to be an effective multikinase inhibitor that could be probably used against brain tumor a...

Reference Reading


1. Flavonoids from Achyrocline satureioides: promising biomolecules for anticancer therapy
Juliana Poglia Carini*, F´ abio Klamt, Valquiria Linck Bassani. RSC Adv.,2014, 4,3131–3144
Flavopiridol is another semisynthetic avonoid with potential anticancer properties. The compound is a flavone derived from rohitukine, a natural anticancer agent isolated from an Indian tree. Due to its interesting biological properties both in vitro and in vivo, as cell cycle arrest in G1 and G2 phases, cytotoxicity against the majority of tumor cell lines in the nanomolar range, suppression of the tumor growth in animals and synergistic activity with most anticancer drugs and radiation, flavopiridol was the first cyclin-dependent kinase (CDK) inhibitor to be tested in human clinical trials. However, the molecule in Phase II clinical trials was ineffective against cancer and presented high toxicity to patients. Nevertheless, currently 60 anticancer clinical trials can be found with flavopiridol, alone or combined with other drugs, whereby 6 of them have shown to be active in the recruiting phase.
2. Mutual interactions between flavonoids and enzymatic and transporter elements responsible for flavonoid disposition via phase II metabolic pathways
Wen Jiang, Ming Hua. RSC Adv., 2012, 2, 7948–7963
Early investigation showed that genistein inhibited the efflux of daunorubicin from small-cell lung cancer GL4/ADR cells, in which MRP was overexpressed, in a competitive manner. The same result of inhibition of daunorubicin by genistein competitively was also observed in plasma membrane vesicles from marine MRP-transfected NIH3T3 cells. Follow-up study confirmed that genistein but not genistin, together with kaempferol and flavopiridol (synthetic flavonoid derivative) could affect MRP-mediated transport of anticancer drugs by a direct interaction with MRP. Moreover, chrysin was reported to inhibit the accumulation of the MRP2 substrate CMFDA in Caco-2 cells in a dose-dependent manner. The maximal accumulation, which could also be achieved by specific MRP inhibitor-MK571, was observed in the presence of 250 mM chrysin. Interestingly, chrysin was also found to increase the expression of MRP2 5 fold in Caco-2 cells after long-term treatment. Over a time period of 48 h, the inhibition of transporter function overtook the enhanced expression of MRP2 by chrysin, resulting in an increased accumulation of topotecan. Therefore, chrysin seemed to play a dual role in regulating MRP2 in Caco-2 cells.