Product Name :
OSI-027 — mTOR Inhibitor
Description:
OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively. It shows more than 100-fold selectivity for mTOR relative to PI3Kα, PI3Kβ, PI3Kγ, and DNA-PK. It inhibits phosphorylation of the mTORC1 substrates 4E-BP1 and S6K1 as well as the mTORC2 substrate AKT in diverse cancer models in vitro and in vivo. OSI-027 shows robust antitumor activity in several different human xenograft models representing various histologies. In COLO 205 and GEO colon cancer xenograft models, OSI-027 showed superior efficacy compared with rapamycin. OSI-027 is currently in Phase I clinical trials in patients with advanced solid tumors or lymphoma.
CAS:
936890-98-1
Molecular Weight:
406.44
Formula:
C21H22N6O3
Chemical Name:
(1r,4r)-4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid
Smiles :
COC1=CC=CC2C=C(NC=21)C1N=C([C@@H]2CC[C@H](CC2)C(O)=O)N2N=CN=C(N)C2=1
InChiKey:
JROFGZPOBKIAEW-HAQNSBGRSA-N
InChi :
InChI=1S/C21H22N6O3/c1-30-15-4-2-3-13-9-14(25-16(13)15)17-18-19(22)23-10-24-27(18)20(26-17)11-5-7-12(8-6-11)21(28)29/h2-4,9-12,25H,5-8H2,1H3,(H,28,29)(H2,22,23,24)/t11-,12-
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
OSI-027 is a selective and potent dual inhibitor of mTORC1 and mTORC2 with IC50 of 22 nM and 65 nM, respectively.{{Estrone} site|{Estrone} Metabolic Enzyme/Protease|{Estrone} Technical Information|{Estrone} Purity|{Estrone} manufacturer|{Estrone} Autophagy} It shows more than 100-fold selectivity for mTOR relative to PI3Kα, PI3Kβ, PI3Kγ, and DNA-PK.{{Thiostrepton} web|{Thiostrepton} Antibiotic|{Thiostrepton} Immunology/Inflammation|{Thiostrepton} Purity & Documentation|{Thiostrepton} In stock|{Thiostrepton} custom synthesis} It inhibits phosphorylation of the mTORC1 substrates 4E-BP1 and S6K1 as well as the mTORC2 substrate AKT in diverse cancer models in vitro and in vivo.PMID:23771862 OSI-027 shows robust antitumor activity in several different human xenograft models representing various histologies. In COLO 205 and GEO colon cancer xenograft models, OSI-027 showed superior efficacy compared with rapamycin. OSI-027 is currently in Phase I clinical trials in patients with advanced solid tumors or lymphoma.|Product information|CAS Number: 936890-98-1|Molecular Weight: 406.44|Formula: C21H22N6O3|Chemical Name: (1r,4r)-4-(4-amino-5-(7-methoxy-1H-indol-2-yl)imidazo[5,1-f][1,2,4]triazin-7-yl)cyclohexanecarboxylic acid|Smiles: COC1=CC=CC2C=C(NC=21)C1N=C([C@@H]2CC[C@H](CC2)C(O)=O)N2N=CN=C(N)C2=1|InChiKey: JROFGZPOBKIAEW-HAQNSBGRSA-N|InChi: InChI=1S/C21H22N6O3/c1-30-15-4-2-3-13-9-14(25-16(13)15)17-18-19(22)23-10-24-27(18)20(26-17)11-5-7-12(8-6-11)21(28)29/h2-4,9-12,25H,5-8H2,1H3,(H,28,29)(H2,22,23,24)/t11-,12-|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO up to 50 mM|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|OSI-027 was used at 1-10 µM in vitro and in cellular assays.|In Vivo:|OSI-027 was orally dosed to mice at 50-65 mg/kg once per day.|References:|Vakana E, et al. Induction of autophagy by dual mTORC1-mTORC2 inhibition in BCR-ABL-expressing leukemic cells. (2010) Autophagy. 6(7):966-7.Carayol N,et al. Critical roles for mTORC2- and rapamycin-insensitive mTORC1-complexes in growth and survival of BCR-ABL-expressing leukemic cells. (2010) Proc Natl Acad Sci USA. 107(28):12469-74.Falcon BL, et al. Reduced VEGF production, angiogenesis, and vascular regrowth contribute to the antitumor properties of dual mTORC1/mTORC2 inhibitors. (2011) Cancer Res. 71(5):1573-83.Products are for research use only. Not for human use.|Documents||
