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Taselisib (GDC 0032) - 99%, high purity , PI3-kinase class I inhibitor, CAS No.1282512-48-4, PI3-kinase class I inhibitor

COA COA
In stock
Item Number
T413710
Grouped product items
SKU Size
Availability
 Price Qty
T413710-5mg
5mg
5
$75.90
T413710-10mg
10mg
5
$118.90
T413710-25mg
25mg
2
$267.90
T413710-100mg
100mg
3
$489.90
Wish List
Bulk Order  SDS  DATASHEET  Specification Sheet

p110δ Selective Inhibitors

View related series
phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit alpha Inhibitor (76) phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit beta Inhibitor (60) phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit delta Inhibitor (71) phosphatidylinositol-4，5-bisphosphate 3-kinase catalytic subunit gamma Inhibitor (69) PI3K (243) PI3K/Akt/mTOR (765)

Basic Description

Synonyms Phenyl chloroformate [UN2746] [Poison] | Taselisib | DB12108 | 1282512-48-4 | Caswell No. 215B | A-dimethyl-1H-pyrazole-1-acetamide | A, | EX-A1581 | HY-13898 | NCGC00387039-02 | SCHEMBL1485247 | Q4272672 | Taselisib (USAN/INN) | UNII-L08J2O299M | BG1662
Specifications & Purity Moligand™, ≥99%
Biochemical and Physiological Mechanisms Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with Ki of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.
Storage Temp Store at -20°C
Shipped In
Ice chest + Ice pads
This product requires cold chain shipping. Ground and other economy services are not available.
Grade Moligand™
Action Type INHIBITOR
Mechanism of action PI3-kinase class I inhibitor
Product Description

Information

Taselisib (GDC 0032, RG7604) is a potent, next-generation β isoform-sparing PI3K inhibitor targetingPI3Kα/δ/γwithKiof 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.


Targets

PI3Kδ (Cell-free assay); PI3Kα (Cell-free assay); PI3Kγ (Cell-free assay); PI3Kβ (Cell-free assay); C2β (Cell-free assay) 14554,0.12 nM(Ki); 0.29 nM(Ki); 0.97 nM(Ki); 9.1 nM(Ki); 292 nM


In vitro

GDC-0032 is an orally bioavailable, potent, and selective inhibitor of Class I PI3Kα, δ, and γ isoforms, with 30 fold less inhibition of the PI3K β isoform relative to the PI3Kα isoform. Preclinical data show that GDC-0032 has increased activity against PI3Kα isoform (PIK3CA) mutant and HER2-amplified cancer cell lines. GDC-0032 inhibits MCF7-neo/HER2 cells proliferation with IC50 of 2.5 nM.


In vivo

GDC-0032 pharmacokinetics is approximately dose proportional and time independent with a mean t1/2 of 40 hours. The combination of GDC-0032 enhances activity of fulvestrant resulting in tumor regressions and tumor growth delay (91% tumor growth inhibition (TGI)). In addition, the combination of GDC-0032 with tamoxifen enhances the efficacy of tamoxifen in vivo (102%TGI for GDC-0032).


Cell Research(from reference)

Cell lines：MCF7-neo/HER2 Cells 

Incubation Time：3 and 4 days 

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
Superclass Organic oxygen compounds
Class Organooxygen compounds
Subclass Ethers
Intermediate Tree Nodes Not available
Direct Parent Alkyl aryl ethers
Alternative Parents N-substituted imidazoles  Benzenoids  Triazoles  Pyrazoles  Heteroaromatic compounds  Primary carboxylic acid amides  Oxacyclic compounds  Azacyclic compounds  Organopnictogen compounds  Organonitrogen compounds  Organic oxides  Hydrocarbon derivatives  Carbonyl compounds  
Molecular Framework Aromatic heteropolycyclic compounds
Substituents Alkyl aryl ether - N-substituted imidazole - Benzenoid - Azole - Imidazole - Heteroaromatic compound - Pyrazole - 1,2,4-triazole - Carboxamide group - Primary carboxylic acid amide - Carboxylic acid derivative - Oxacycle - Azacycle - Organoheterocyclic compound - Hydrocarbon derivative - Organic nitrogen compound - Organic oxide - Organonitrogen compound - Organopnictogen compound - Carbonyl group - Aromatic heteropolycyclic compound
Description This compound belongs to the class of organic compounds known as alkyl aryl ethers. These are organic compounds containing the alkyl aryl ether functional group with the generic formula R-O-R' , where R is an alkyl group and R' is an aryl group.
External Descriptors Not available

Product Properties

ALogP 2.47
HBD Count 1
Rotatable Bond 5

Associated Targets(Human)

PIK3CG Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PIK3CA Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform (5 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PIK3CB Tchem Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
PIK3CD Tclin Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform (3 Activities)
Activity Type Activity Value -log(M) Mechanism of Action Activity Reference Publications (PubMed IDs)
ABL1 Tclin Tyrosine-protein kinase ABL (18331 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PRKDC Tchem DNA-dependent protein kinase (1929 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
GSK3B Tclin Glycogen synthase kinase-3 beta (11785 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CSNK1D Tchem Casein kinase I delta (4546 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3CD Tclin PI3-kinase p110-delta subunit (6699 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
MTOR Tclin Serine/threonine-protein kinase mTOR (13850 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3CG Tclin PI3-kinase p110-gamma subunit (5411 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3CB Tchem PI3-kinase p110-beta subunit (4044 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
AURKA Tchem Serine/threonine-protein kinase Aurora-A (10240 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PC-3 (62116 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
U2OS (164939 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HepG2 (196354 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3C2B Tchem Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing beta polypeptide (438 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Liver (3974 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3C3 Tchem Phosphatidylinositol 3-kinase catalytic subunit type 3 (535 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
PIK3C2A Tchem Phosphatidylinositol-4-phosphate 3-kinase C2 domain-containing subunit alpha (139 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRD4 Tchem Bromodomain-containing protein 4 (13122 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
TRIM24 Tchem Transcription intermediary factor 1-alpha (2087 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
BRPF1 Tchem Peregrin (2217 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
HEK-293T (167025 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Associated Targets(non-human)

PIK3CA PI3-kinase p110-alpha subunit (51 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mapk1 MAP kinase ERK2 (650 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Hdac6 Histone deacetylase 6 (222 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Fgfr3 Fibroblast growth factor receptor 3 (21 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Mus musculus (284745 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID
Plasma (328 Activities)
Activity Type Relation Activity value Units Action Type Journal PubMed Id doi Assay Aladdin ID

Mechanisms of Action

Mechanism of Action Action Type target ID Target Name Target Type Target Organism Binding Site Name References

Names and Identifiers

Pubchem Sid 504771000
Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/504771000
IUPAC Name 2-methyl-2-[4-[2-(5-methyl-2-propan-2-yl-1,2,4-triazol-3-yl)-5,6-dihydroimidazo[1,2-d][1,4]benzoxazepin-9-yl]pyrazol-1-yl]propanamide
INCHI InChI=1S/C24H28N8O2/c1-14(2)32-22(27-15(3)29-32)19-13-30-8-9-34-20-10-16(6-7-18(20)21(30)28-19)17-11-26-31(12-17)24(4,5)23(25)33/h6-7,10-14H,8-9H2,1-5H3,(H2,25,33)
InChIKey BEUQXVWXFDOSAQ-UHFFFAOYSA-N
Smiles CC1=NN(C(=N1)C2=CN3CCOC4=C(C3=N2)C=CC(=C4)C5=CN(N=C5)C(C)(C)C(=O)N)C(C)C
Isomeric SMILES CC1=NN(C(=N1)C2=CN3CCOC4=C(C3=N2)C=CC(=C4)C5=CN(N=C5)C(C)(C)C(=O)N)C(C)C
PubChem CID 51001932
Molecular Weight 460.53

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:

Find and download the COA for your product by matching the lot number on the packaging.

8 results found

Lot Number Certificate Type Date Item
F2230495 Certificate of Analysis Apr 07, 2025 T413710
F2230496 Certificate of Analysis Apr 07, 2025 T413710
F2310596 Certificate of Analysis Nov 28, 2022 T413710
F2310600 Certificate of Analysis Nov 28, 2022 T413710
F2310601 Certificate of Analysis Nov 28, 2022 T413710
F2310599 Certificate of Analysis Nov 28, 2022 T413710
F2310605 Certificate of Analysis Nov 28, 2022 T413710
F2310606 Certificate of Analysis Nov 28, 2022 T413710

Chemical and Physical Properties

Solubility Solubility (25°C) In vitro DMSO: 70 mg/mL warmed with 50ºC Water: bath (151.99 mM); Ethanol: 7 mg/mL warmed with 50ºC Water: bath (15.19 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility 70
DMSO(mM) Max Solubility 151.998784
Water(mg / mL) Max Solubility ＜1
Molecular Weight 460.500 g/mol
XLogP3 1.800
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 6
Rotatable Bond Count 5
Exact Mass 460.234 Da
Monoisotopic Mass 460.234 Da
Topological Polar Surface Area 119.000 Ų
Heavy Atom Count 34
Formal Charge 0
Complexity 750.000
Isotope Atom Count 0
Defined Atom Stereocenter Count 0
Undefined Atom Stereocenter Count 0
Defined Bond Stereocenter Count 0
Undefined Bond Stereocenter Count 0
The total count of all stereochemical bonds 0
Covalently-Bonded Unit Count 1

Alternative Products

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    Taselisib (GDC 0032), PI3-kinase class I inhibitor

    Starting at $241.90

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