venetoclax - CAS 1257044-40-8
Catalog number: B0084-462638
Category: Inhibitor
Please be kindly noted products are not for therapeutic use. We do not sell to patients.
Molecular Formula:
C45H50ClN7O7S
Molecular Weight:
868.44
COA:
Inquire
Targets:
Bcl-2 Family
Description:
Venetoclax is a small-molecule inhibitor that has high selectivity for Bcl-2 (Ki < 0.01 nM in cell-free assays) over Mcl-1. It suppresses anti-apoptotic Bcl-2, a protein commonly overexpressed in cancer cells, to induce programmed death of CLL cells. Venetoclax is used as a second-line treatment of chronic lymphocytic leukemia (CLL).
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-462638 500 mg $298 In stock
Bulk Inquiry
Brife Description:
Bcl-2 inhibitor, chronic lymphocytic leukemia (CLL)
Synonyms:
Venclexta; ABT-199
Solubility:
10mM in DMSO
MSDS:
Inquire
Application:
the treatment of chronic lymphocytic leukemia (CLL)
Shelf Life:
2 years
InChIKey:
LQBVNQSMGBZMKD-UHFFFAOYSA-N
InChI:
InChI=1S/C45H50ClN7O7S/c1-45(2)15-11-33(39(26-45)31-3-5-34(46)6-4-31)29-51-17-19-52(20-18-51)35-7-9-38(42(24-35)60-36-23-32-12-16-47-43(32)49-28-36)44(54)50-61(57,58)37-8-10-40(41(25-37)53(55)56)48-27-30-13-21-59-22-14-30/h3-10,12,16,23-25,28,30,48H,11,13-15,17-22,26-27,29H2,1-2H3,(H,47,49)(H,50,54)
Canonical SMILES:
CC1(CCC(=C(C1)C2=CC=C(C=C2)Cl)CN3CCN(CC3)C4=CC(=C(C=C4)C(=O)NS(=O)(=O)C5=CC(=C(C=C5)NCC6CCOCC6)[N+](=O)[O-])OC7=CN=C8C(=C7)C=CN8)C
Current Developer:
AbbVie; Genentech
1.BCR signaling inhibitors differ in their ability to overcome Mcl-1-mediated resistance of CLL B cells to ABT-199.
Bojarczuk K1, Sasi BK1, Gobessi S1, Innocenti I2, Pozzato G3, Laurenti L2, Efremov DG4. Blood. 2016 Apr 19. pii: blood-2015-10-675009. [Epub ahead of print]
The Bcl-2 antagonist ABT-199 has demonstrated promising clinical activity in patients with CLL. ABT-199 is strongly cytotoxic against unstimulated peripheral blood CLL cellsin vitro, but is much less effective against CLL cells that have received survival signals from the microenvironment. In particular, stimulation of CLL cells with CD40L results in substantial resistance that is mediated by induction of the antiapoptotic Bcl-2 family proteins Bcl-xLand Bfl-1. In the present study we investigated whether resistance to ABT-199 can be conferred by B-cell receptor (BCR) stimulation, which is another important survival signal from the leukemic microenvironment. We show that sustained BCR stimulation results in significant ABT-199-resistance, which correlates with induction of the antiapoptotic protein Mcl-1 and less consistently with downregulation of proapoptotic Bmf, Hrk and BimEL A major role for Mcl-1 in conferring ABT-199 resistance is additionally supported by knockdown and enforced expression experiments with primary CLL cells.
2.Binding of released Bim to Mcl-1 is a mechanism of intrinsic resistance to ABT-199 which can be overcome by combination with daunorubicin or cytarabine in AML cells.
Niu X1, Zhao J2, Ma J1, Xie C3, Edwards H4, Wang G1, Caldwell JT5, Xiang S6, Zhang X7, Chu R8, Wang J9, Lin H10, Taub JW11, Ge Y12. Clin Cancer Res. 2016 Apr 21. pii: clincanres.3057.2015. [Epub ahead of print]
PURPOSE: To investigate the molecular mechanism underlying intrinsic resistance to ABT-199.
3.Complementary dynamic BH3 profiles predict co-operativity between the multi-kinase inhibitor TG02 and the BH3 mimetic ABT-199 in acute myeloid leukaemia cells.
Pallis M1, Burrows F2, Ryan J3, Grundy M1, Seedhouse C4, Abdul-Aziz A4, Montero J3, Letai A3, Russell N1,4. Oncotarget. 2016 Apr 15. doi: 10.18632/oncotarget.8742. [Epub ahead of print]
Direct co-operation between sensitiser molecules BAD and NOXA in mediating apoptosis suggests that therapeutic agents which sensitise to BAD may complement agents which sensitise to NOXA. Dynamic BH3 profiling is a novel methodology that we have applied to the measurement of complementarity between sensitiser BH3 peptide mimetics and therapeutic agents. Using dynamic BH3 profiling, we show that the agent TG02, which downregulates MCL-1, sensitises to the BCL-2-inhibitory BAD-BH3 peptide, whereas the BCL-2 antagonist ABT-199 sensitises to MCL-1 inhibitory NOXA-BH3 peptide in acute myeloid leukaemia (AML) cells. At the concentrations used, the peptides did not trigger mitochondrial outer membrane permeabilisation in their own right, but primed cells to release Cytochrome C in the presence of an appropriate trigger of a complementary pathway. In KG-1a cells TG02 and ABT-199 synergised to induce apoptosis. In heterogeneous AML patient samples we noted a range of sensitivities to the two agents.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related Bcl-2 Family Products


CAS 12542-36-8 Gossypol Acetic Acid

Gossypol Acetic Acid
(CAS: 12542-36-8)

The Acetate acid salt form of gossypol which may represent a promising new anticancer agent with a novel molecular mechanism and warrants further investigation ...

CAS 329349-20-4 Bax channel blocker

Bax channel blocker
(CAS: 329349-20-4)

Bax channel blocker is a potent inhibitor of Bax-mediated mitochondrial cytochrome c release (IC50 = 0.52 μM).

CAS 65673-63-4 HA14-1

HA14-1
(CAS: 65673-63-4)

HA14-1 is a potent Bcl-2 inhibitor with potential anticancer activity. HA14-1 induces apoptosis in various human cancer cells. HA14-1 suppressed NF-kappaB activ...

CAS 2752-65-0 Gambogic acid

Gambogic acid
(CAS: 2752-65-0)

Gambogic acid is a natural product inhibitor of Hsp90.

CAS 1235034-55-5 A-1155463

A-1155463
(CAS: 1235034-55-5)

A-1155463, an effective and selective BCL-XL inhibitor, has been studied to have probable effect in restraining the growth of small cell lung cancer xenograft t...

A-1210477
(CAS: 1668553-26-1)

A-1210477 is a potent and selective MCL-1 inhibitor with Ki and IC50 of 0.454 nM and 26.2 nM, respectively, >100-fold selectivity over other Bcl-2 family member...

WEHI-539
(CAS: 1431866-33-9)

WEHI-539, a selective BCL-XL inhibitor that can be function as a single-agent inducer of apoptosis while sparing normal cells, it leads to MOMP and apoptosis du...

Marinopyrrole A
(CAS: 1227962-62-0)

Marinopyrrole A, a new Mcl-1 inhibitor, could influence Mcl-1-Bim interaction and induce the degradation of Mcl-1 proteasomal and also lead to the apoptosis of ...

CAS 1426138-42-2 FX1

FX1
(CAS: 1426138-42-2)

FX1 is a selective inhibitor of B cell lymphoma 6 (BCL6) (IC50 = 35 μM in reporter assays), which can disrupt formation of the BCL6 repression complex, reactiva...

CAS 518303-20-3 UMI-77

UMI-77
(CAS: 518303-20-3)

UMI-77 is a selective Mcl-1 inhibitor with Ki of 490 nM, showing selectivity over other members of Bcl-2 family.

CAS 579492-81-2 Bax inhibitor peptide V5

Bax inhibitor peptide V5
(CAS: 579492-81-2)

Bax inhibitor peptide V5, a peptide inhibitor, as a pro-apoptotic member of Bcl-2 family proteins and plays an important role in mitochondria-dependent apoptosi...

CAS 38778-30-2 Muristerone A

Muristerone A
(CAS: 38778-30-2)

Muristerone A, a phytoecdysteroid analog of ecdysone, acts as an inducer of ecdysone-inducible gene expression systems in mammalian cells and transgenic animals...

Mcl1-IN-2
(CAS: 292057-76-2)

Mcl1-IN-2, a hydroxyquinoline derivative, is an Mcl-1 inhibitor.

Spautin-1
(CAS: 1262888-28-7)

Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM.

CAS 90141-22-3 AT101

AT101
(CAS: 90141-22-3)

AT101, the R-(-) enantiomer of Gossypol acetic acid, binds with Bcl-2, Bcl-xL and Mcl-1 with Ki of 0.32 μM, 0.48 μM and 0.18 μM.

Bak BH3

Bak BH3, derived from the BH3 domain of Bak, was found to antagonize the protective effects of microinjected Bcl-xL in a-Fas-treated HeLa cells, whereas a mutan...

CAS 866541-93-7 AT-101 acetic acid

AT-101 acetic acid
(CAS: 866541-93-7)

AT101 acetic acid is orally bioavailable solvate of R-(-)-enantiomer of gossypol with potential antineoplastic activity. It is used as the treatment of non Hodg...

CAS 303-45-7 Gossypol

Gossypol
(CAS: 303-45-7)

Gossypol is an orally-active polyphenolic aldehyde with potential antineoplastic activity. Derived primarily from unrefined cottonseed oil, gossypol induces cel...

CAS 1430844-80-6 A-1331852

A-1331852
(CAS: 1430844-80-6)

A-1331852, a substituted benzothiazole, is a high affinity BH3 mimetic Ligand of BCL protein BCL-XL (Ki≤ 10 pM). A-1331852 is an orally apoptosis-inducing agent...

CAS 852808-04-9 ABT-737

ABT-737
(CAS: 852808-04-9)

ABT-737 is a potent, cell-permeable mimetic of BH3 domains that avidly binds Bcl-2, Bcl-xL, and Bcl-W (Ki < 1 nM for all three proteins). It blocks the interact...

Chemical Structure

CAS 1257044-40-8 venetoclax

Quick Inquiry

Verification code

Featured Items