Grouped product items

SKU

Size

Availability

Price

Qty

A124869-5mg

5mg

In stock

$58.90

A124869-10mg

10mg

In stock

$82.90

A124869-25mg

25mg

In stock

$94.90

A124869-50mg

50mg

In stock

$105.90

A124869-100mg

100mg

In stock

$137.90

A124869-500mg

500mg

In stock

$621.90

Basic Description

Synonyms	Venetoclax\|1257044-40-8\|ABT-199\|Venclexta\|GDC-0199\|ABT199\|ABT 199\|venclyxto\|RG7601\|UNII-N54AIC43PW\|GDC 0199\|RG-7601\|Venetoclax (ABT199)\|N54AIC43PW\|Venetoclax; Abt-199\|Venetoclax(ABT-199)\|4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperaz
Specifications & Purity	Moligand™, ≥99%
Biochemical and Physiological Mechanisms	ABT-199 is a potent and selective inhibitor of B-cell lymphoma-2 (BCL-2) family proteins, currently in clinical trials. ABT-199 inhibits the growth of BCL-2-dependent tumors in vivo and spares human platelets. A single dose of ABT-199 in three patients wi
Storage Temp	Protected from light,Store at -20°C
Shipped In	Ice chest + Ice pads
Grade	Moligand™
Action Type	ANTAGONIST, INHIBITOR
Mechanism of action	Apoptosis regulator Bcl-2 inhibitor
Product Description	ABT-199 (GDC-0199) is a BH3 mimetic that Bcl-2-selective inhibitor with Ki of <0.01 nM. B-cell lymphoma/leukemia 2 (Bcl-2) is an anti-apoptotic protein that controls cell survival by binding the BH3 domains of pro-death BAD and BAK proteins and preventing permeabilization of the mitochondrial outer membrane. This protein is tightly regulated for the homeostasis between cell growth and cell death. A Bcl-2-selective inhibitor with Ki of <0.01 nM

Product Properties

ALogP	8.2

Associated Targets

DRD1 Tclin D(1A) dopamine receptor 0 Activities

Discover Target: DRD1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

Discover Target: BRD4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

Discover Target: CDK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

Discover Target: FGFR3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

HRH1 Tclin Histamine H1 receptor 0 Activities

Discover Target: HRH1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

Discover Target: CSNK1D

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A2 Tclin Sodium-dependent noradrenaline transporter 0 Activities

Discover Target: SLC6A2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A3 Tclin Sodium-dependent dopamine transporter 0 Activities

Discover Target: SLC6A3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

SLC6A4 Tclin Sodium-dependent serotonin transporter 0 Activities

Discover Target: SLC6A4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

Discover Target: TRIM24

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PGR Tclin Progesterone receptor 0 Activities

Discover Target: PGR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDE4D Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4D 0 Activities

Discover Target: PDE4D

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PDE3A Tclin cGMP-inhibited 3',5'-cyclic phosphodiesterase A 0 Activities

Discover Target: PDE3A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PTGS1 Tclin Prostaglandin G/H synthase 1 0 Activities

Discover Target: PTGS1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PTGS2 Tclin Prostaglandin G/H synthase 2 0 Activities

Discover Target: PTGS2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MCL1 Tchem Induced myeloid leukemia cell differentiation protein Mcl-1 1 Activities

Discover Target: MCL1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MC3R Tchem Melanocortin receptor 3 0 Activities

Discover Target: MC3R

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NR1I2 Tchem Nuclear receptor subfamily 1 group I member 2 0 Activities

Discover Target: NR1I2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CASP3 Tchem Caspase-3 0 Activities

Discover Target: CASP3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BRPF1 Tchem Peregrin 0 Activities

Discover Target: BRPF1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BAD Tchem Bcl2-associated agonist of cell death 0 Activities

Discover Target: BAD

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BCL2 Tclin Apoptosis regulator Bcl-2 10 Activities

Discover Target: BCL2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AURKA Tchem Aurora kinase A 0 Activities

Discover Target: AURKA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BCL2L1 Tchem Bcl-2-like protein 1 10 Activities

Discover Target: BCL2L1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

BCL2L2 Tchem Bcl-2-like protein 2 2 Activities

Discover Target: BCL2L2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

DRD3 Tclin D(3) dopamine receptor 0 Activities

Discover Target: DRD3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRB2 Tclin Beta-2 adrenergic receptor 0 Activities

Discover Target: ADRB2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADRA2C Tclin Alpha-2C adrenergic receptor 0 Activities

Discover Target: ADRA2C

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

Discover Target: ABL1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CHRM1 Tclin Muscarinic acetylcholine receptor M1 0 Activities

Discover Target: CHRM1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AR Tclin Androgen receptor 0 Activities

Discover Target: AR

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAOA Tclin Amine oxidase [flavin-containing] A 0 Activities

Discover Target: MAOA

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ADORA3 Tchem Adenosine receptor A3 0 Activities

Discover Target: ADORA3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ASPH Tchem Aspartyl/asparaginyl beta-hydroxylase 0 Activities

Discover Target: ASPH

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

Discover Target: GSK3B

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Discover Target: KCNH2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

OPRD1 Tclin Delta-type opioid receptor 0 Activities

Discover Target: OPRD1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Discover Target: MAPK1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Names and Identifiers

Pubchem Sid	488201440
Pubchem Sid Url	https://pubchem.ncbi.nlm.nih.gov/substance/488201440
IUPAC Name	4-[4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohexen-1-yl]methyl]piperazin-1-yl]-N-[3-nitro-4-(oxan-4-ylmethylamino)phenyl]sulfonyl-2-(1H-pyrrolo[2,3-b]pyridin-5-yloxy)benzamide
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)
InChi Key	LQBVNQSMGBZMKD-UHFFFAOYSA-N
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
Isomeric 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
PubChem CID	49846579
Molecular Weight	868.44

Database links

CAS Registry No.	1257044-40-8
PubChem CID	49846579
ChEMBL Ligand	CHEMBL3137309
RCSB PDB Ligand	LBM
DrugCentral Ligand	5133
PubChem SID	488201440

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

To view the certificate results,please click on a Lot number.For Lot numbers from past orders,please use our order status section

17 results found

Lot Number	Certificate Type	Date	Item
K2208012	Certificate of Analysis	Aug 22, 2024	A124869
K2208013	Certificate of Analysis	Aug 22, 2024	A124869
K2208014	Certificate of Analysis	Aug 22, 2024	A124869
K2208015	Certificate of Analysis	Aug 22, 2024	A124869
E2224032	Certificate of Analysis	Mar 18, 2024	A124869
C1608065	Certificate of Analysis	Aug 08, 2023	A124869
I2122116	Certificate of Analysis	Jul 10, 2023	A124869
I2122117	Certificate of Analysis	Jul 10, 2023	A124869
E2320102	Certificate of Analysis	May 11, 2023	A124869
E2320108	Certificate of Analysis	May 11, 2023	A124869
E2320109	Certificate of Analysis	May 11, 2023	A124869
E2320112	Certificate of Analysis	May 11, 2023	A124869
E2320113	Certificate of Analysis	May 11, 2023	A124869
E2320114	Certificate of Analysis	May 11, 2023	A124869
E2322580	Certificate of Analysis	May 11, 2023	A124869
C2302802	Certificate of Analysis	Mar 15, 2023	A124869
K2208016	Certificate of Analysis	Oct 26, 2022	A124869

Chemical and Physical Properties

Solubility	Soluble in DMSO (100 mg/ml (~115mM) at 25 °C), water (<1 mg/ml (< 1mM) at 25 °C), and ethanol (<1 mg/ml (< 1mM) at 25 °C).
Sensitivity	light sensitive
Refractive Index	1.64

Safety and Hazards(GHS)

Pictogram(s)	GHS08, GHS07
Signal	Danger
Hazard Statements	H315:Causes skin irritation H319:Causes serious eye irritation H335:May cause respiratory irritation H302:Harmful if swallowed H372:Causes damage to organs through prolonged or repeated exposure H361:Suspected of damaging fertility or the unborn child
Precautionary Statements	P261:Avoid breathing dust/fume/gas/mist/vapors/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing. P280:Wear protective gloves/protective clothing/eye protection/face protection. P302+P352:IF ON SKIN: wash with plenty of water. P321:Specific treatment (see ... on this label). P405:Store locked up. P501:Dispose of contents/container to ... P264:Wash hands [and …] thoroughly after handling. P260:Do not breathe dust/fume/gas/mist/vapors/spray. P271:Use only outdoors or in a well-ventilated area. P270:Do not eat, drink or smoke when using this product. P304+P340:IF INHALED: Remove person to fresh air and keep comfortable for breathing. P403+P233:Store in a well-ventilated place. Keep container tightly closed. P362+P364:Take off contaminated clothing and wash it before reuse. P330:Rinse mouth. P203:Obtain, read and follow all safety instructions before use. P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes. P301+P317:IF SWALLOWED: Get medical help. P318:if exposed or concerned, get medical advice. P337+P317:If eye irritation persists: Get medical help. P332+P317:If skin irritation occurs: Get medical help. P319:Get medical help if you feel unwell.

FAQs and Articles

FAQ

GDC-1971: SHP2 Inhibitor Ushering in a New Era of Cancer Treatment

Categories: Technical articles

Tags:

Building Blocks Inhibitors drug target ligand GDC-1971 SHP2 KRAS

References

1. Souers AJ, Leverson JD, Boghaert ER, Ackler SL, Catron ND, Chen J, Dayton BD, Ding H, Enschede SH, Fairbrother WJ et al.. (2013) ABT-199, a potent and selective BCL-2 inhibitor, achieves antitumor activity while sparing platelets.. Nat Med, 19 (2): (202-8). [PMID:23291630]
2. Tian BP, Xia LX, Bao ZQ, Zhang H, Xu ZW, Mao YY, Cao C, Che LQ, Liu JK, Li W et al.. (2017) Bcl-2 inhibitors reduce steroid-insensitive airway inflammation.. J Allergy Clin Immunol, 140 (2): (418-430). [PMID:28043871]
3. Seymour JF, Kipps TJ, Eichhorst B, Hillmen P, D'Rozario J, Assouline S, Owen C, Gerecitano J, Robak T, De la Serna J et al.. (2018) Venetoclax-Rituximab in Relapsed or Refractory Chronic Lymphocytic Leukemia.. N Engl J Med, 378 (12): (1107-1120). [PMID:29562156]

Solution Calculators

Molarity Calculator

Determine the necessary mass, volume, or concentration for preparing a solution.

Dilution Calculator

Determine the dilution needed to prepare a stock solution.

ABT-199 (GDC-0199) - ≥99%, high purity , Apoptosis regulator Bcl-2 inhibitor, CAS No.1257044-40-8, Apoptosis regulator Bcl-2 inhibitor

Basic Description

Product Properties

Associated Targets

DRD1 Tclin D(1A) dopamine receptor 0 Activities

BRD4 Tchem Bromodomain-containing protein 4 0 Activities

CDK2 Tchem Cyclin-dependent kinase 2 0 Activities

FGFR3 Tclin Fibroblast growth factor receptor 3 0 Activities

HRH1 Tclin Histamine H1 receptor 0 Activities

CSNK1D Tchem Casein kinase I isoform delta 0 Activities

SLC6A2 Tclin Sodium-dependent noradrenaline transporter 0 Activities

SLC6A3 Tclin Sodium-dependent dopamine transporter 0 Activities

SLC6A4 Tclin Sodium-dependent serotonin transporter 0 Activities

TRIM24 Tchem Transcription intermediary factor 1-alpha 0 Activities

PGR Tclin Progesterone receptor 0 Activities

PDE4D Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4D 0 Activities

PDE3A Tclin cGMP-inhibited 3',5'-cyclic phosphodiesterase A 0 Activities

PTGS1 Tclin Prostaglandin G/H synthase 1 0 Activities

PTGS2 Tclin Prostaglandin G/H synthase 2 0 Activities

MCL1 Tchem Induced myeloid leukemia cell differentiation protein Mcl-1 1 Activities

MC3R Tchem Melanocortin receptor 3 0 Activities

NR1I2 Tchem Nuclear receptor subfamily 1 group I member 2 0 Activities

CASP3 Tchem Caspase-3 0 Activities

BRPF1 Tchem Peregrin 0 Activities

BAD Tchem Bcl2-associated agonist of cell death 0 Activities

BCL2 Tclin Apoptosis regulator Bcl-2 10 Activities

AURKA Tchem Aurora kinase A 0 Activities

BCL2L1 Tchem Bcl-2-like protein 1 10 Activities

BCL2L2 Tchem Bcl-2-like protein 2 2 Activities

DRD3 Tclin D(3) dopamine receptor 0 Activities

ADRB2 Tclin Beta-2 adrenergic receptor 0 Activities

ADRA2C Tclin Alpha-2C adrenergic receptor 0 Activities

ABL1 Tclin Tyrosine-protein kinase ABL1 0 Activities

CHRM1 Tclin Muscarinic acetylcholine receptor M1 0 Activities

AR Tclin Androgen receptor 0 Activities

MAOA Tclin Amine oxidase [flavin-containing] A 0 Activities

ADORA3 Tchem Adenosine receptor A3 0 Activities

ASPH Tchem Aspartyl/asparaginyl beta-hydroxylase 0 Activities

GSK3B Tclin Glycogen synthase kinase-3 beta 0 Activities

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

OPRD1 Tclin Delta-type opioid receptor 0 Activities

MAPK1 Tchem Mitogen-activated protein kinase 1 0 Activities

Names and Identifiers

Database links

Certificates

Certificate of Analysis(COA)

more

Chemical and Physical Properties

Safety and Hazards(GHS)

Related Documents

FAQs and Articles

References

Solution Calculators

Molarity Calculator

Dilution Calculator

Reconstitution Calculator