en

Targeted-Oncology


Product Name: Format/Size Descriptions Download
Targeted Oncology Library 4815 compounds
For cherry-picking
Update: 2020-07
The file contains all available Targeted-Oncology compounds selected from our Signature & BioDesign Libraries.
SL#029
IDH inhibitors - Cancer Metabolism
80 compounds
Pre-Plated Set
Release: 2016
Identified pharmacophore features of known IDH inhibitors and a subsequent search across the ASINEX corporate collection has revealed several quinolone-based analogs available at ASINEX. With these compounds as a starting point, ASINEX has applied its medicinal chemistry expertise in creating an array of novel small molecules potentially interesting for IDH-related research.
SL#043
State1(T) inhibitors of activated Ras
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has identified several rigid analogs of BPA that are able to coordinate with Metal(II) ions and can therefore be exploited as chemical probes for Ras-related research.
SL#053
Katanin inhibitors
80 compounds
Pre-Plated Set
Release: 2016
2D similarity search through ASINEX’s compound collection identified several close analogs of known katanin inhibitors that could be interesting for katanin-related research and MTA drug discovery.
SL#066
Inhibitors of miсroRNA-21
80 compounds
Pre-Plated Set
Release: 2017
Small molecules that can bind directly to microRNA-21 (miR-21) have been suggested as a promising new therapy for the treatment of cancer. Screening a large library of drug-like small molecules has identified several chemotypes that bind to the pre-miR-21 hairpin with high selectivity against other oligonucleotides. The most potent hit molecules share the common 1-amino-3-(9H-carbazol-9-yl)propan-2-ol scaffold which can be considered a privileged fragment. 80 molecules containing this privileged fragment were included in this library.
SL#071
Taxol pharmacophore chemical probes
80 compounds
Pre-Plated Set
Release: 2017
80 close analogs of the reported hits have been included in this library.
SL#085
Tubulin Inhibitors
80 compounds
Pre-Plated Set
Release: 2018
A series of novel phenoxazine and phenothiazine derivatives have been recently reported as privileged chemotypes in the discovery and development of novel tubulin polymerization inhibitors. Computational studies suggested that these compounds bind to β-tubulin at the colchicine binding site. Structural analogs of the reported hit series were included into this library.
SL#087
elF4A3 inhibitors
80 compounds
Pre-Plated Set
Release: 2018
A series of 5-(piperazine-1-carbonyl)pyridin-2(1H)-one derivatives have been identified as useful probe molecules for studying the eIF4A3 cell biology and exploring its therapeutic potential in cancer models. A similarity search through ASINEX’s compound collection identified several analogs of the reported inhibitors.

You may also like:

Product Name: Format/Size Descriptions Download
SL#003
Wnt/β-catenin Pathway Inhibitors
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has screened 21000 small molecules in a luciferase reporter assay using the colorectal cancer cell lines, SW620 (APC mutation) and HCT116 (GSK3b mutation). Selected primary hits were optimized to yield an array of active compounds showing EC50 0.1-5 uM. The most promising compounds down regulate the expression of the key WNT oncogenes: DKK, cycD, CD44.
SL#001
Mcl-1 Apoptosis
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has developed several acylsulfonamide derivatives with Mcl-1 binding potency and improved physico-chemical characteristics.
SL#002
Bcl-xL Apoptosis
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has identified dihydrobenzofurane as a functional a-helix mimetic displaying uM Bcl-xL binding affinity determined by a fluorescence polarization assay.
SL#011
MDM2-p53 (α-Helix mimetics)
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has performed in-silico analyses of common structural futures of known MDM2 antagonists to build up a predictive pharmacophore model [1]. Several ɑ-helix mimetic scaffolds were selected as p53 backbone mimetics and p53 binding epitope mimetics [2,3]. The in vitro potency of compounds was confirmed in a fluorescence polarization assay, with the IC50s ranging from 1 to 10 µM.
Product Name: Format/Size Descriptions Download
Immuno-Oncology Library 6334 compounds
For cherry-picking
Update: 2020-07
The file contains all available Immuno-Oncology compounds selected from our Signature & BioDesign Libraries.
SL#021
IDO1 inhibitors
80 compounds
Pre-Plated Set
Release: 2016
By utilizing a combination of scaffold hopping and structure-based design strategies ASINEX has developed a library of small molecules for IDO1 drug discovery. Selected compounds have shown significant IDO1 inhibitory activity in vitro as measured in the enzymatic biochemical assays.
SL#026
IRAK4 inhibitors
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has created a series of IRAK4-oriented compounds by combining the IRAK4 hinge binding motif with proprietary natural product-like fragments. Several compounds from this library were screened against IRAK4 kinase in vitro and showed sub-uM IC50. Sunitinib was also included in the library as a reference compound.
SL#033
PD1/PD-L1 inhibitors
80 compounds
Pre-Plated Set
Release: 2016
ASINEX has designed a set of novel small molecule probes that can be used for exploration of PD-1/PD-L1 signaling pathway.
Phenotypic Screening Sets: Format/Size Descriptions Download
Phenotypic Pre-Plated Set 13159 compounds
Pre-Plated Set
Amount: 0.01-2.0 mg
Update: 2020-07
ASINEX has created a diverse set of molecules by applying strict physico-chemical and structural descriptors to ensure good solubility and permeability properties.
Asinex in GOSTAR 1878 compounds
41742 analogues
For cherry-picking
Update: 2020-11
Asinex have opted to use the Global Online Structure Activity Relationship Database (GOSTAR) as an integrated source of data capturing chemical, biological, pharmacological, and therapeutic parameters. The structural overlap between the Asinex (500K+) and GOSTAR (8M+) databases has revealed 17910 unique molecules with associated biological activity. Application of additional structural filters (PAINS, Eli Lilly [4-5]) has resulted in a set of 11923 compounds; diversity-oriented selection supported by computational and medicinal chemistry expertise has further refined this set resulting in 1878 molecules available for computational or in vitro evaluation. Biological diversity is represented by multiple target families where each molecule is associated with a GOSTAR record via a unique structure code identifier.
SL#004
Oncology Phenotypic Screening-1
(Non-Macrocycle)
80 compounds / set
Pre-Plated Set
Update: 2016
ASINEX's oncology-oriented phenotypic library includes compounds based on several scaffolds with proven cytotoxicity (sub-µM EC50 in MTT assay) against a number of cancer cell lines: MV-411 (acute monocytic leukemia), HCT-116 (human colon cancer), MCF-7 (human breast adenocarcinoma‎), A-172 (Human glioblastoma), COLO-320 (colorectal adenocarcinoma), U-937 (histiocytic lymphoma), A-375 (malignant melanoma), BXPC-3 (pancreas adenocarcinoma), U118-MG (malignant glioma), and LN-229 (glioblastoma). Some active compounds were screened in a biochemical assay showing nM level of IC50 against several kinases: Aurora A, Haspin, VEGFR, EGFR, PDGFR.
SL#023
Oncology Phenotypic Screening-2
(Colon Cancer/Non-Macrocycle)
80 compounds / set
Pre-Plated Set
Update: 2016
ASINEX has evaluated the susceptibility of several colon cancer cell lines (HCT-116, SW-620, COLO-320, RKO) to a diverse array of small molecules and identified a series of related compounds that kill cancer cells at sub-µM concentrations with limited off target effect on healthy cells (human fibroblasts). Additional screening in a cell-based luciferase reporter assay of Wnt signaling has provided preliminary evidence of Wnt-dependent mechanism of action.
SL#035
Oncology Phenotypic Screening-3
(Macrocycles)
80 compounds / set
Pre-Plated Set
Update: 2016
ASINEX has evaluated the susceptibility of several cancer cell lines (i.e. RKO, HCT116, Molt-4, Rs4-11, U937, A549, H1568, H23, PANC1, A2780) to an array of peptidic and non-peptidic macrocycles and identified a series of compounds that kill cancer cells at µM concentrations.
Contact
Global

Ludmila Sadovenko

lsadovenko@asinex.com
North America

Mark Parisi

mparisi@asinex.com

Toll Free: +1 877 ASINEX1

Tel: +1 336 721 1617

Fax: +1 336 721 1618

N.Chestnut St., Ste.104

Winston-Salem, NC 27101

USA

Europe

Galina Afanasyeva

gafanasyeva@asinex.com

Tel: +31 (0) 203416183

Klaprozenweg 75C, 1033NN

Amsterdam, The Netherlands

Japan

Shingo Ota

sota@asinex.com

Tel: 080-3401-9097

30-2 Higashihazu, Nishio,

Aichi Japan

Cart
Your cart is empty
Order
$
0
Checkout
Thanks for your order
We will contact you shortly