AD80 - CAS 1384071-99-1
Category: Inhibitor
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Molecular Formula:
C22H19F4N7O
Molecular Weight:
473.43
COA:
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Targets:
Others
Description:
AD80, also called as A-196, is a multikinase inhibitor that inhibits against human BRAF, S6K, and SRC and shows strong activity against RET inhibitor.
Brife Description:
A multikinase inhibitor
Synonyms:
1-[4-(4-amino-1-propan-2-ylpyrazolo[3,4-d]pyrimidin-3-yl)phenyl]-3-[2-fluoro-5-(trifluoromethyl)phenyl]urea; AD-80; s8518
Solubility:
DMSO: ≥ 150 mg/mL
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
Inquire
Boiling Point:
530.9±50.0 ℃ at 760 Torr
Density:
1.49±0.1 g/cm3
InChIKey:
CYORWDWRQMVGHN-UHFFFAOYSA-N
InChI:
1S/C22H19F4N7O/c1-11(2)33-20-17(19(27)28-10-29-20)18(32-33)12-3-6-14(7-4-12)30-21(34)31-16-9-13(22(24,25)26)5-8-15(16)23/h3-11H,1-2H3,(H2,27,28,29)(H2,30,31,34)
Canonical SMILES:
CC(C)N1C2=C(C(=N1)C3=CC=C(C=C3)NC(=O)NC4=C(C=CC(=C4)C(F)(F)F)F)C(=NC=N2)N
1.Use of synthetic polypeptides in the preparation of biodegradable delivery vehicles for narcotic antagonists.
Sidman KR;Arnold DL;Steber WD;Nelsen L;Granchelli FE;Strong P;Sheth SG Natl Inst Drug Abuse Res Monogr Ser. 1976 Jan;(4):33-8.
Synthetic polypeptides consisting of copolymers of glutamic acid and leucine have been shown to be useful materials for the fabrication of practical, biodegradable delivery vehicles for narcotic antagonists. Model delivery vehicles in film form were prepared from copolymers containing 10 mole percent to 40 mole percent glutamic acid, and loaded with 10% to 40% naltrexone by weight. The naltrexone was found to be released by diffusion, exhibiting diffusion coefficients that varied as a function of the glutamic acid content and the initial naltrexone loading. A wide range in diffusion coefficients were achieved (0.31 x 10-7 cm2/hr to 120 x 10-7 cm2/hr), leading to release rates within practical ranges of interest for meeting the program goals. We have demonstrated that the polypeptides can be fabricated into dosage forms that are amenable to administration by trochar. For example, rods 0.4 mm to 0.8 mm in diameter containing as much as 40% naltrexone by weight were extruded using a simple compression mold and die arrangement. An in vitro evaluation of the rods showed that antagonist is released by diffusion at a continuously decreasing rate, a behavior similar to that observed with the film devices that were, nonetheless, capable of blocking an AD80 challenge of morphene sulfate in mice for more than 30 days.
2.Use of synthetic polypeptides in the preparation of biodegradable delivery vehicles for narcotic antagonists.
Sidman KR;Arnold DL;Steber WD;Nelsen L;Granchelli FE;Strong P;Sheth SG Natl Inst Drug Abuse Res Monogr Ser. 1975;(4):33-8.
Synthetic polypeptides consisting of copolymers of glutamic acid and leucine have been shown to be useful materials for the fabrication of practical, biodegradable delivery vehicles for narcotic antagonists. Model delivery vehicles in film form were prepared from copolymers containing 10 mole percent to 40 mole percent glutamic acid, and loaded with 10% to 40% naltrexone by weight. The naltrexone was found to be released by diffusion, exhibiting diffusion coefficients that varied as a function of the glutamic acid content and the initial naltrexone loading. A wide range in diffusion coefficients were achieved (0.31 x 10(-7) cm2/hr to 120 x 10(-7) cm2/hr), leading to release rates within practical ranges of interest for meeting the program goals. We have demonstrated that the polypeptides can be fabricated into dosage forms that are amenable to administration by trochar. For example, rods 0.4 mm to 0.8 mm in diameter containing as much as 40% naltrexone by weight were extruded using a simple compression mold and die arrangement. An in vitro evaluation of the rods showed that antagonist is released by diffusion at a continuously decreasing rate, a behavior similar to that observed with the film devices that were, nonetheless, capable of blocking an AD80 challenge of morphine sulfate in mice for more than 30 days.
3.Drugging the catalytically inactive state of RET kinase in RET-rearranged tumors.
Plenker D;Riedel M;Brägelmann J;Dammert MA;Chauhan R;Knowles PP;Lorenz C;Keul M;Bührmann M;Pagel O;Tischler V;Scheel AH;Schütte D;Song Y;Stark J;Mrugalla F;Alber Y;Richters A;Engel J;Leenders F;Heuckmann JM;Wolf J;Diebold J;Pall G;Peifer M;Aerts M;Gevaert K;Zahedi RP;Buettner R;Shokat KM;McDonald NQ;Kast SM;Gautschi O;Thomas RK;Sos ML Sci Transl Med. 2017 Jun 14;9(394). pii: eaah6144. doi: 10.1126/scitranslmed.aah6144.
Oncogenic fusion events have been identified in a broad range of tumors. Among them, ;RET; rearrangements represent distinct and potentially druggable targets that are recurrently found in lung adenocarcinomas. We provide further evidence that current anti-RET drugs may not be potent enough to induce durable responses in such tumors. We report that potent inhibitors, such as AD80 or ponatinib, that stably bind in the DFG-out conformation of RET may overcome these limitations and selectively kill ;RET;-rearranged tumors. Using chemical genomics in conjunction with phosphoproteomic analyses in ;RET;-rearranged cells, we identify the CCDC6-RET;I788N; mutation and drug-induced mitogen-activated protein kinase pathway reactivation as possible mechanisms by which tumors may escape the activity of RET inhibitors. Our data provide mechanistic insight into the druggability of RET kinase fusions that may be of help for the development of effective therapies targeting such tumors.
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CAS 1384071-99-1 AD80

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