Determine the necessary mass, volume, or concentration for preparing a solution.
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
SKU | Size | Availability | Price | Qty |
---|---|---|---|---|
G414217-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $345.90 | |
G414217-10mg | 10mg | In stock | $593.90 | |
G414217-25mg | 25mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $1,187.90 | |
G414217-50mg | 50mg | In stock | $1,880.90 |
RIP kinase Inhibitors
Synonyms | BCP31015 | 5-benzyl-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-1H-1,2,4-triazole-3-carboxamide | EX-A3069 | (S)-5-Benzyl-N-(7,9-difluoro-2-oxo-2,3,4,5-tetrahydro-1hbenzo(b)azepin-3-yl)-1H-1,2,4-triazole-3-carboxamide (7,7-dimethyl-2- |
---|---|
Specifications & Purity | Moligand™, ≥99% |
Biochemical and Physiological Mechanisms | GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Grade | Moligand™ |
Action Type | INHIBITOR |
Mechanism of action | Inhibitor of receptor interacting serine/threonine kinase 1 |
Product Description | Information GSK3145095 GSK3145095 is a potent and orally active RIP1 kinase inhibitor with IC50 of 6.3 nM with potential antineoplastic and immunomodulatory activities. Targets RIP1 kinase (Cell-free assay) 6.3 nM In vitro GSK3145095 potently binds to RIP1 with exquisite kinase specificity and has excellent activity in blocking RIP1 kinasedependent cellular responses. Highlighting its potential as a novel cancer therapy, the inhibitor is also able to promote a tumor suppressive T cell phenotype in pancreatic adenocarcinoma organ cultures. Cell Research(from reference) Cell lines:U937 cells, L-cells NCTC 929 (L929) cells Concentrations:0-3 μM Incubation Time:5 h |
ALogP | 2.573 |
---|---|
HBD Count | 3 |
Rotatable Bond | 4 |
Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
---|
IUPAC Name | 5-benzyl-N-[(3S)-7,9-difluoro-2-oxo-1,3,4,5-tetrahydro-1-benzazepin-3-yl]-1H-1,2,4-triazole-3-carboxamide |
---|---|
INCHI | InChI=1S/C20H17F2N5O2/c21-13-9-12-6-7-15(19(28)25-17(12)14(22)10-13)23-20(29)18-24-16(26-27-18)8-11-4-2-1-3-5-11/h1-5,9-10,15H,6-8H2,(H,23,29)(H,25,28)(H,24,26,27)/t15-/m0/s1 |
InChi Key | ATQAGKAMBISZQM-HNNXBMFYSA-N |
Canonical SMILES | C1CC2=C(C(=CC(=C2)F)F)NC(=O)C1NC(=O)C3=NNC(=N3)CC4=CC=CC=C4 |
Isomeric SMILES | C1CC2=C(C(=CC(=C2)F)F)NC(=O)[C@H]1NC(=O)C3=NNC(=N3)CC4=CC=CC=C4 |
PubChem CID | 118557502 |
Molecular Weight | 397.38 |
Solubility | Solubility (25°C) In vitro DMSO: 79 mg/mL (198.8 mM); Ethanol: 6 mg/mL (15.09 mM); Water: Insoluble; |
---|---|
DMSO(mg / mL) Max Solubility | 79 |
DMSO(mM) Max Solubility | 198.802154109417 |
Water(mg / mL) Max Solubility | <1 |
1. Harris PA, Marinis JM, Lich JD, Berger SB, Chirala A, Cox JA, Eidam PM, Finger JN, Gough PJ, Jeong JU et al.. (2019) Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer.. ACS Med Chem Lett, 10 (6): (857-862). [PMID:31223438] [10.1021/op500134e] |