N-[(3R)-3-(2-chloro-5-fluorophenyl)-6-(5-cyano-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-1-oxo-2,3-dihydroisoindol-4-yl]-3-fluoro-5-(trifluoromethyl)benzamide manufacturers
- RLY-2608
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- $132.00
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2026-07-27
- CAS:2733573-94-7
- Purity: 99.87%
- Supply Ability: 10g
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| | N-[(3R)-3-(2-chloro-5-fluorophenyl)-6-(5-cyano-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-1-oxo-2,3-dihydroisoindol-4-yl]-3-fluoro-5-(trifluoromethyl)benzamide Basic information |
| Product Name: | N-[(3R)-3-(2-chloro-5-fluorophenyl)-6-(5-cyano-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-1-oxo-2,3-dihydroisoindol-4-yl]-3-fluoro-5-(trifluoromethyl)benzamide | | Synonyms: | N-[(3R)-3-(2-chloro-5-fluorophenyl)-6-(5-cyano-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-1-oxo-2,3-dihydroisoindol-4-yl]-3-fluoro-5-(trifluoromethyl)benzamide;N-[(3R)-3-(2-chloro-5-fluoro-phenyl)-6-(5-cyano-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-1-oxo-isoindolin-4-yl]-3-fluoro-5-(trifluoromethyl)benzamide;(R)-N-(3-(2-Chloro-5-fluorophenyl)-6-(5-cyano-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-1-oxoisoindolin-4-yl)-3-fluoro-5-(trifluoromethyl)benzamide;RLY2608;zovegalisib | | CAS: | 2733573-94-7 | | MF: | C29H14ClF5N6O2 | | MW: | 608.91 | | EINECS: | | | Product Categories: | | | Mol File: | 2733573-94-7.mol | ![N-[(3R)-3-(2-chloro-5-fluorophenyl)-6-(5-cyano-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-1-oxo-2,3-dihydroisoindol-4-yl]-3-fluoro-5-(trifluoromethyl)benzamide Structure](CAS/20210305/GIF/2733573-94-7.gif) |
| | N-[(3R)-3-(2-chloro-5-fluorophenyl)-6-(5-cyano-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-1-oxo-2,3-dihydroisoindol-4-yl]-3-fluoro-5-(trifluoromethyl)benzamide Chemical Properties |
| density | 1.61±0.1 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted) | | form | Solid | | pka | 11.06±0.40(Predicted) | | color | White to off-white | | InChIKey | VYWRYBZVVSPTQN-SANMLTNESA-N | | SMILES | C(NC1=CC(C2=C(C#N)N3N=CN=C3C=C2)=CC2=C1[C@H](C1=CC(F)=CC=C1Cl)NC2=O)(=O)C1=CC(C(F)(F)F)=CC(F)=C1 |
| | N-[(3R)-3-(2-chloro-5-fluorophenyl)-6-(5-cyano-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-1-oxo-2,3-dihydroisoindol-4-yl]-3-fluoro-5-(trifluoromethyl)benzamide Usage And Synthesis |
| Uses | RLY-2608 is an orally active first-in-class allosteric mutant-selective inhibitor of PI3Ka with anti-tumor activity. RLY-2608 inhibits tumor growth in PIK3CA-mutant xenograft mice models with minimal impact on insulin[1][2][3]. | | in vivo | RLY-2608 (25-100 mg/kg, p.o., twice a day for 50 days) inhibits tumors in tumor xenograft mice models with reduced impact on insulin levels[1].
RLY-2608 (12.5-100 mg/kg, p.o., a single dose for 4 days) demonstrates potent tumor growth inhibition in Balb/c nude female mice bearing HSC-2 tumors[2].
| Animal Model: | Tumor xenograft mice models[1] | | Dosage: | 25-100 mg/kg | | Administration: | p.o., twice a day for 50 days | | Result: | Potentiated tumor regression in tumor xenograft mice models. |
| | References | [1] Andreas Varkaris, et al. Discovery and clinical proof-of-concept of RLY-2608, a first-in-class mutant-selective allosteric PI3Ka inhibitor that decouples anti-tumor activity from hyperinsulinemia. Cancer Discov. 2023 Nov 2. DOI:10.1158/2159-8290.CD-23-0944
[2] Pazolli E, et al. RLY-2608: the first allosteric mutant-and isoform-selective inhibitor of PI3Kα, is efficacious as a single agent and drives regressions in combination with standard of care therapies in PIK3CA mutant breast cancer models[J]. Cancer Res., 2022, 82.
[3] Perez C A, et al. First-in-human global multi-center study of RLY-2608, a pan-mutant and isoform-selective PI3Kα inhibitor, as a single agent in patients with advanced solid tumors and in combination with fulvestrant in patients with advanced breast cancer[J]. 2022. |
| | N-[(3R)-3-(2-chloro-5-fluorophenyl)-6-(5-cyano-[1,2,4]triazolo[1,5-a]pyridin-6-yl)-1-oxo-2,3-dihydroisoindol-4-yl]-3-fluoro-5-(trifluoromethyl)benzamide Preparation Products And Raw materials |
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