1,2,5-Thiadiazolidin-3-one, 5-[(7R)-1-fluoro-5,6,7,8-tetrahydro-3-hydroxy-7-[(3-methylbutyl)amino]-2-naphthalenyl]-, 1,1-dioxide
- Product Name
- 1,2,5-Thiadiazolidin-3-one, 5-[(7R)-1-fluoro-5,6,7,8-tetrahydro-3-hydroxy-7-[(3-methylbutyl)amino]-2-naphthalenyl]-, 1,1-dioxide
- CAS No.
- 2489404-97-7
- Chemical Name
- 1,2,5-Thiadiazolidin-3-one, 5-[(7R)-1-fluoro-5,6,7,8-tetrahydro-3-hydroxy-7-[(3-methylbutyl)amino]-2-naphthalenyl]-, 1,1-dioxide
- Synonyms
- ABBV-CLS-484;A-484;Osunprotafib;ABBV-CLS-484 ,E1207;Osunprotafib (ABBV-CLS-484);AC 484|||Osunprotafib|||AC484|||ABBV-CLS-484;5-[(3R)-5-fluoro-7-hydroxy-3-(isopentylamino)tetralin-6-yl]-1,1-dioxo-1,2,5-thiadiazolidin-3-one;(R)-5-(1-Fluoro-3-hydroxy-7-(isopentylamino)-5,6,7,8-tetrahydronaphthalen-2-yl)-1,2,5-thiadiazolidin-3-one 1,1-dioxide;1,2,5-Thiadiazolidin-3-one, 5-[(7R)-1-fluoro-5,6,7,8-tetrahydro-3-hydroxy-7-[(3-methylbutyl)amino]-2-naphthalenyl]-, 1,1-dioxide
- CBNumber
- CB49811227
- Molecular Formula
- C17H24FN3O4S
- Formula Weight
- 385.45
- MOL File
- 2489404-97-7.mol
1,2,5-Thiadiazolidin-3-one, 5-[(7R)-1-fluoro-5,6,7,8-tetrahydro-3-hydroxy-7-[(3-methylbutyl)amino]-2-naphthalenyl]-, 1,1-dioxide Property
- Density
- 1.41±0.1 g/cm3(Predicted)
- pka
- 3.39±0.20(Predicted)
- form
- Solid
- color
- White to light yellow
- InChI
- InChI=1S/C17H24FN3O4S/c1-10(2)5-6-19-12-4-3-11-7-14(22)17(16(18)13(11)8-12)21-9-15(23)20-26(21,24)25/h7,10,12,19,22H,3-6,8-9H2,1-2H3,(H,20,23)/t12-/m1/s1
- InChIKey
- DVFCRTGTEXUFIN-GFCCVEGCSA-N
- SMILES
- S1(=O)(=O)N(C2=C(O)C=C3C(=C2F)C[C@H](NCCC(C)C)CC3)CC(=O)N1
1,2,5-Thiadiazolidin-3-one, 5-[(7R)-1-fluoro-5,6,7,8-tetrahydro-3-hydroxy-7-[(3-methylbutyl)amino]-2-naphthalenyl]-, 1,1-dioxide Chemical Properties,Usage,Production
Uses
Osunprotafib (ABBV-CLS-484) is a potent PTPN1 and PTPN2 inhibitor with subnanomolar activity. Osunprotafib has antitumor activity, enhances the immune response and increases the sensitivity of tumors to immune-mediated killing[1].
in vivo
Osunprotafib promotes anti-tumor immunity as a monotherapy and, when combined with anti-PD-1, leads to significant tumor regression, even in models resistant to anti-PD-1 treatment, such as 4T1 and EMT6[3].
References
[1] Philip R. Kym, et al. Protein tyrosine phosphatase inhibitors and methods of use thereof. WO2022056281A1.
[2] Arvin Iracheta-Vellve, et al. Targeting the immune checkpoint PTPN2 with ABBV-CLS-484 inflames the tumor microenvironment and unleashes potent CD8+ T cell immunity. Cancer Res (2022) 82 (12_Supplement): 606.
[3] Christina K, et al. ABBV-CLS-484: An active site PTPN2/N1 inhibitor that augments the immune response and sensitizes tumors to immune-mediated killing. Cancer Res (2022) 82 (12_Supplement): ND06.
1,2,5-Thiadiazolidin-3-one, 5-[(7R)-1-fluoro-5,6,7,8-tetrahydro-3-hydroxy-7-[(3-methylbutyl)amino]-2-naphthalenyl]-, 1,1-dioxide Preparation Products And Raw materials
Raw materials
Preparation Products
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