AT7519 trifluoroacetate - CAS 1431697-85-6
Catalog number: 1431697-85-6
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C18H18Cl2F3N5O4
Molecular Weight:
496.27
COA:
Inquire
Targets:
CDK
Description:
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 = 89 nM). AT7519 shows potent antiproliferative activity in a variety of human tumor cell lines with IC50 values ranging from 40 nM for MCF-7 to 940 nM for SW620 consistent with the inhibition of CDK1 and CDK2. AT7519 induces dose-dependent cytotoxicity in multiple myeloma (MM) cell lines with IC50 values ranging from 0.5 to 2 μM at 48 hours, with the most sensitive cell lines being MM.1S (0.5 μM) and U266 (0.5 μM) and the most resistant MM.1R (>2 μM). It does not induce cytotoxicity in peripheral blood mononuclear cells (PBMNC). AT7519 partially overcomes the proliferative advantage conferred by IL6 and IGF-1 as well as the protective effect of bone marrow stromal cells (BMSCs). AT7519 induces rapid dephosphorylation of RNA pol II CTD at serine 2 and serine 5 sites, and leads to the inhibition of transcription, partially contributing to AT7519 induced cytotoxicity of MM cells. AT7519 induces activation of GSK-3β by down-regulating GSK-3β phosphorylation, which also contributes to AT7519 induced apoptosis independent of the inhibition of transcription. A twice daily dosing of AT7519 (9.1 mg/kg) causes tumor regression of both early-stage and advanced-stage s.c. tumors in the HCT116 and HT29 colon cancer xenograft models. AT7519 treatment (15 mg/kg) inhibits tumor growth and prolongs the median overall survival of mice in the human MM xenograft mouse model in association with increased caspase 3 activation.
Publictions citing BOC Sciences Products
  • >> More
Purity:
>98%
Synonyms:
AT 7519 trifluoroacetate; AT-7519 trifluoroacetate
MSDS:
Inquire
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related CDK Products


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...

CAS 902135-91-5 AT7519 HCl

AT7519 HCl
(CAS: 902135-91-5)

CAS 131740-09-5 Flavopiridol Hydrochloride

Flavopiridol Hydrochloride
(CAS: 131740-09-5)

Flavopiridol hydrochloride competes with ATP to inhibit CDKs including CDK1, CDK2, CDK4 and CDK6 with IC50 of ~ 40 nM. It is 7.5-fold more selective for CDK1/2/...

CAS 1374639-79-8 LEE011 succinate hydrate

LEE011 succinate hydrate
(CAS: 1374639-79-8)

LEE011 succinate hydrate is an orally available cyclin-dependent kinase (CDK) inhibitor targeting cyclin D1/CDK4 and cyclin D3/CDK6 cell cycle pathway, with pot...

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 920113-03-7 Riviciclib HCl

Riviciclib HCl
(CAS: 920113-03-7)

Riviciclib, also known as P276-00, is a novel CDK1, CDK4 and CDK9 inhibitor with IC50 of 79 nM, 63 nM and 20 nM, respectively. P276-00 selectively binds to and ...

CAS 844442-38-2 AT-7519

AT-7519
(CAS: 844442-38-2)

AT-7519 is an orally bioavailable small molecule CDK inhibitor with potential antineoplastic activity. AT7519M selectively binds to and inhibits cyclin dependen...

CAS 1619903-54-6 LY2857785

LY2857785
(CAS: 1619903-54-6)

LY2857785 is a potent and selective CDK9 inhibitor; significantly reduces RNAP II CTD phosphorylation and dramatically decreases MCL1 protein levels to result i...

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...

CCT-251921
(CAS: 1607837-31-9)

CCT-251921 has been found to be a CDK inhibitor that could be significant in the studies of colorectal cancer.

CAS 1092443-52-1 BS181

BS181
(CAS: 1092443-52-1)

BS-181 is a highly selective CDK inhibitor for CDK7 with an IC(50) of 21 nmol/L. Testing of other CDKs as well as another 69 kinases showed that BS-181 only inh...

CGP74514A
(CAS: 190653-73-7)

CGP74514A is a cell permeable Cdk inhibitor selective for Cyclin-dependent kinase-1 (Cdk1) (IC50=25nM). CGP74514A was also reported also to affect the activitie...

Senexin A
(CAS: 1366002-50-7)

Senexin A is a selective Cell division protein kinase 8 (CDK8) inhibitor with IC50 value of 280 nM. Senexin A can bind to cdk19 in an ATP-competitive manner and...

CAS 1374639-75-4 LEE011 succinate

LEE011 succinate
(CAS: 1374639-75-4)

LEE011 is an orally bioavailable and highly specific CDK4/6 (cyclin-dependent kinase 4/6) inhibitor. LEE011 in combination with LGX818 (a V600E BRAF specific in...

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 143621-35-6 Triapine

Triapine
(CAS: 143621-35-6)

3-Aminopyridine-2-carboxaldehyde thiosemicarbazone (3-AP) is a ribonucleotide reductase inhibitor and iron chelator with anti-tumor activity.

CAS 212844-54-7 Purvalanol B

Purvalanol B
(CAS: 212844-54-7)

Purvalanol B is a cyclin-dependent; 2,6,9-substituted kinase inhibitor.

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 1211443-80-9 LEE011 hydrochloride

LEE011 hydrochloride
(CAS: 1211443-80-9)

CDK4/6 inhibitor LEE011 specifically inhibits CDK4 and 6, thereby inhibiting retinoblastoma (Rb) protein phosphorylation. Inhibition of Rb phosphorylation preve...

Chemical Structure

CAS 1431697-85-6 AT7519 trifluoroacetate

Quick Inquiry

Verification code

Featured Items