GSK3145095
GSK3145095 is a potent and orally active RIPK1 inhibitor (IC50 = 5 nM) with potential antineoplastic and immunomodulatory activities. GSK3145095 disrupts RIPK1-mediated signaling, which may reduce C-X-C motif chemokine ligand 1 (CXCL1)-driven recruitment and migration of immunosuppressive myeloid-derived suppressor cells (MDSCs) in the tumor microenvironment (TME). This allows effector cells, such as natural killer (NK) cells and cytotoxic T lymphocytes (CTLs), to kill and eliminate cancer cells. GSK3145095 is currently under clinical trails.
For research use only. We do not sell to patients.
Chemical Information
| Name | GSK3145095 |
|---|---|
| Iupac Chemical Name | (S)-5-benzyl-N-(7,9-difluoro-2-oxo-2,3,4,5-tetrahydro-1H-benzo[b]azepin-3-yl)-4H-1,2,4-triazole-3-carboxamide |
| Synonyms | GSK3145095; GSK-3145095; GSK 3145095; |
| Molecular Formula | C20H17F2N5O2 |
| Molecular Weight | 397.3858 |
| Smile | O=C(C1=NN=C(CC2=CC=CC=C2)N1)N[C@H]3CCC4=CC(F)=CC(F)=C4NC3=O |
| InChiKey | ATQAGKAMBISZQM-HNNXBMFYSA-N |
| 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 |
| CAS Number | 1622849-43-7 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Solid powder |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
Identification of a RIP1 Kinase Inhibitor Clinical Candidate (GSK3145095) for the Treatment of Pancreatic Cancer
Philip A. Harris, Jill M. Marinis, John D. Lich, Scott B. Berger, Anirudh Chirala, Julie A. Cox, Patrick M. Eidam, Joshua N. Finger, Peter J. Gough, Jae U. Jeong, James Kang, Viera Kasparcova, Lara K. Leister, Mukesh K. Mahajan, George Miller, Rakesh Nagilla, Michael T. Ouellette, Michael A. Reilly, Alan R. Rendina, Elizabeth J. Rivera, Helen H. Sun, James H. Thorpe, Rachel D. Totoritis, Wei Wang, Dongling Wu, Daohua Zhang, John Bertin, and Robert W. Marquis
Publication Date (Web): May 9, 2019 (Featured Letter)
DOI: 10.1021/acsmedchemlett.9b00108
Chemical Structure
