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PI3K/AKT/mTOR
PI3K
PI3K
下级目录
5-(7-(Methylsulfonyl)-2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine
[5-[2,4-Bis((3S)-3-methylmorpholin-4-yl)pyrido[2,3-d]pyrimidin-7-yl]-2-methoxyphenyl]methanol
Apitolisib
AT13148
Debio-0932 (CUDC305)
Capivasertib
CZC24832
N-[4-[[4-(Dimethylamino)-1-piperidinyl]carbonyl]phenyl]-N'-[4-[4,6-di(4-morpholinyl)-1,3,5-triazin-2-yl]phenyl]urea
(2S)-N1-[4-Methyl-5-[2-(2,2,2-trifluoro-1,1-dimethylethyl)-4-pyridinyl]-2-thiazolyl]-1,2-pyrrolidinedicarboxamide
CAY10505
GSK-2256098
ETP-46321
CNX-1351
HS-173
PI3K/HDACInhibitor
BAY1082439
GNE-317
ISA-2011B
AMG-319
AZD8186
2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
A-443654
Chidamide
Acalisib
CAL-101
Golvatinib
GSK1059615
(-)-Deguelin
KRX-0601
AS-604850
Gsk-690693
目录项下的产品
1007207-67-1 / MFCD107207671
CH5132799, also known as PA-799, is a novel class I PI3K inhibitor, which exhibited a strong inhibitory activity especially against PI3Kα (IC(50)=0.014 μM). In human tumor cell lines with PI3K pathway activation, CH5132799 showed potent antiproliferative activity. CH5132799 is orally available and showed significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice. CH5132799 selectively inhibited class I PI3Ks and PI3Kα mutants in in vitro kinase assays. Tumors harboring PIK3CA mutations were significantly sensitive to CH5132799 in vitro and were remarkably regressed by CH5132799 in in vivo mouse xenograft models.
CH5132799
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0
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0.0
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中华人民共和国
1009298-09-2 / MFCD109298092
Azd-8055
[5-[2,4-二((3S)-3-甲基吗啉-4-基)吡啶并[2,3-D]嘧啶-7-基]-2-甲氧基苯基]甲醇
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0
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0.0
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0.0
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中华人民共和国
√
1032754-93-0 / MFCD132754930
Apitolisib
(S)-1-(4-((2-(2-氨基嘧啶-5-基)-7-甲基-4-吗啉代噻吩并[3,2-d]嘧啶-6-基)甲基)哌嗪-1-基)-2-羟基丙-1-酮
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0
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0.0
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0.0
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1056901-62-2 / MFCD156901622
AT13148 is a novel oral multi-AGC kinase inhibitor with potent pharmacodynamic and antitumor activity, which shows a distinct mechanism of action from other AKT inhibitors. AT13148 is currently being developed by Astex Pharmaceuticals. AT131148 was identified utilizing high-throughput X-ray crystallography and fragment-based lead discovery techniques. AT13148 caused substantial blockade of AKT, p70S6K, PKA, ROCK and SGK substrate phosphorylation and induction of apoptosis in both a concentration and time-dependent manner in cancer cells with clinically relevant genetic defects both in vitro and in vivo.
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1061318-81-7 / MFCD161318817
Debio-0932 (CUDC305)
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0
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0.0
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0.0
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1143532-39-1 / MFCD243532391
(S)-4-Amino-N-(1-(4-Chlorophenyl)-3-Hydroxypropyl)-1-(7H-Pyrrolo[2,3-D]Pyrimidin-4-Yl)Piperidine-4-Carboxamide
(S)-4-氨基-N-(1-(4-氯苯基)-3-羟丙基)-1-(7H-吡咯并[2,3-d]嘧啶-4-基)哌啶-4-甲酰胺
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0
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1159824-67-5 / MFCD259824675
CZC24832 is the first selective inhibitor of phosphoinositide 3-kinase γ (PI3Kγ) with efficacy in in vitro and in vivo models of inflammation. Extensive target- and cell-based profiling of CZC24832 revealed regulation of interleukin-17-producing T helper cell (T(H)17) differentiation by PI3Kγ, thus reinforcing selective inhibition of PI3Kγ as a potential treatment for inflammatory and autoimmune diseases.
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1197160-78-3 / MFCD297160783
1-(4-(4-(Dimethylamino)Piperidine-1-Carbonyl)Phenyl)-3-(4-(4,6-Dimorpholino-1,3,5-Triazin-2-Yl)Phenyl)Urea
1-(4-(4-(二甲氨基)哌啶-1-羰基)苯基)-3-(4-(4,6-二吗啉-1,3,5-三嗪-2-基)苯基)脲
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1217486-61-7 / MFCD317486617
Alpelisib, also known as BLY719, is an orally bioavailable phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor BYL719 specifically inhibits PIK3 in the PI3K/AKT kinase (or protein kinase B) signaling pathway, thereby inhibiting the activation of the PI3K signaling pathway. This may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Activation of the PI3K signaling pathway is frequently associated with tumorigenesis. Dysregulated PI3K signaling may contribute to tumor resistance to a variety of antineoplastic agents. Check for active clinical trials or closed clinical trials using this agent.
(2S)-N1-[4-甲基-5-[2-(2,2,2-三氟-1,1-二甲基乙基)-4-吡啶基]-2-噻唑基]-1,2-吡咯烷二甲酰胺
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0
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0.0
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0.0
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中华人民共和国
√
1218777-13-9 / MFCD318777139
(E)-5-((5-(4-Fluorophenyl)furan-2-yl)methylene)thiazolidine-2,4-dione
(E)-5-((5-(4-氟苯基)呋喃-2-基)亚甲基)噻唑烷-2,4-二酮
原料
0
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0.0
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0.0
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中华人民共和国
1224887-10-8 / MFCD324887108
2-((5-Chloro-2-((1-Isopropyl-3-Methyl-1H-Pyrazol-5-Yl)Amino)Pyridin-4-Yl)Amino)-N-Methoxybenzamide
2-((5-氯-2-((1-异丙基-3-甲基-1H-吡唑-5-基)氨基)吡啶-4-基)氨基)-N-甲氧基苯甲酰胺
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0
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0.0
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0.0
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中华人民共和国
1252594-99-2 / MFCD352594992
ETP-46321
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0
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0.0
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0.0
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1276105-89-5 / MFCD376105895
CNX-1351 is a selective covalent Inhibitor of PI3Kα. In an end point assay, CNX-1351 potently inhibited PI3Kα and was 20−400 times less potent against β, γ, and δ. CNX-1351 inhibit PI3Kα signaling in cells and shows prolonged inhibition consistent with a covalent mechanism of Action. CNX-1351 inhibits growth of cells dependent on PI3Kα. CNX-1351 also inhibits PI3Kα signaling in vivo and bonds to p110α.
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1276110-06-5 / MFCD376110065
Ethyl 6-(5-(Phenylsulfonamido)Pyridin-3-Yl)Imidazo[1,2-A]Pyridine-3-Carboxylate
6-(5-(苯基磺酰胺基)吡啶-3-基)咪唑并[1,2-a]吡啶-3-羧酸乙酯
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0
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0.0
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1339928-25-4 / MFCD439928254
N-Hydroxy-2-(((2-(6-Methoxypyridin-3-Yl)-4-Morpholinothieno[3,2-D]Pyrimidin-6-Yl)Methyl)(Methyl)Amino)Pyrimidine-5-Carboxamide
N-羟基-2-(((2-(6-甲氧基吡啶-3-基)-4-吗啉噻吩并[3,2-d]嘧啶-6-基)甲基)(甲基)氨基)嘧啶-5-甲酰胺
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1375469-38-7 / MFCD475469387
BAY1082439 is an orally bioavailable inhibitor of the class I phosphoinositide 3-kinase (PI3K) alpha and beta isoforms with potential antineoplastic activity. PI3K alpha/beta inhibitor BAY1082439 selectively inhibits both PI3K alpha, including mutated forms of PIK3CA, and PI3K beta in the PI3K/Akt/mTOR pathway, which may result in tumor cell apoptosis and growth inhibition in PI3K-expressing and/or PTEN-driven tumor cells. By specifically targeting class I PI3K alpha and beta, this agent may be more efficacious and less toxic than pan PI3K inhibitors.
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1394076-92-6 / MFCD494076926
GNE-317
GNE-317游离态
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1395347-24-6 / MFCD495347246
ISA-2011B is a PIP5Kα (Phosphatidylinositol-4-phosphate 5-kinase-α) inhibitor. The overexpression of PIP5K1α is associated with poor prognosis in prostate cancer and correlates with an elevated level of the androgen receptor. ISA-2011B significantly inhibits growth of tumor cells in xenograft mice, which is mediated by targeting PIP5K1α-associated PI3K/AKT and the downstream survival, proliferation, and invasion pathways. PIP5K1α has high potential as a drug target, and compound ISA-2011B is interesting for further development of targeted cancer therapy.
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1608125-21-8 / MFCD708125218
(S)-N-(1-(7-Fluoro-2-(pyridin-2-yl)quinolin-3-yl)ethyl)-9H-purin-6-amine
(S)-N-(1-(7-氟-2-(吡啶-2-基)喹啉-3-基)乙基)-9H-嘌呤-6-胺
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1627494-13-6 / MFCD727494136
(R)-8-(1-((3,5-Difluorophenyl)Amino)Ethyl)-N,N-Dimethyl-2-Morpholino-4-Oxo-4H-Chromene-6-Carboxamide
(R)-8-(1-((3,5-二氟苯基)氨基)乙基)-N,N-二甲基-2-吗啉-4-氧代-4H-苯并吡喃-6-甲酰胺
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371242-69-2 / MFCD71242692
2-[(6-Amino-9H-purin-9-yl)methyl]-5-methyl-3-(2-methylphenyl)-4(3H)-quinazolinone
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552325-16-3 / MFCD52325163
A-443654
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0
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0.0
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743420-02-2 / MFCD43420022
Chidamide
N-(2-氨基-5-氟苯基)-4-((3-(吡啶-3-基)丙烯酰氨基)甲基)苯甲酰胺
原料
0
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0.0
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0.0
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中华人民共和国
870281-34-8 / MFCD70281348
(S)-2-(1-((9H-Purin-6-Yl)Amino)Ethyl)-6-Fluoro-3-Phenylquinazolin-4(3H)-One
(S)-2-(1-((9H-嘌呤-6-基)氨基)乙基)-6-氟-3-苯基喹唑啉-4(3H)-酮
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870281-82-6 / MFCD70281826
5-Fluoro-3-phenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4(3H)-quinazolinone
5-氟-3-苯基-2-[(1S)-1-(9H-嘌呤-6-基氨基)丙基]-4(3H)-喹唑啉酮
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中华人民共和国
北京市
√
928037-13-2 / MFCD028037132
N-(2-Fluoro-4-((2-(4-(4-Methylpiperazin-1-Yl)Piperidine-1-Carboxamido)Pyridin-4-Yl)Oxy)Phenyl)-N-(4-Fluorophenyl)Cyclopropane-1,1-Dicarboxamide
N-[2-氟-4-[[2-[[[4-(4-甲基哌嗪-1-基)哌啶-1-基]羰基]氨基]吡啶-4-基]氧基]苯基]-N'-(4-氟苯基)环丙烷-1,1-二甲酰胺
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958852-01-1 / MFCD058852011
GSK1059615 is a phosphoinositide 3-kinase (PI3K) inhibitor with potential antineoplastic activity. PI3K inhibitor GSK1059615 inhibits PI3K in the PI3K/AKT kinase signaling pathway, which may trigger the translocation of cytosolic Bax to the mitochondrial outer membrane and an increase in mitochondrial membrane permeability, followed by apoptosis. Bax is a member of the proapoptotic Bcl-2 family of proteins. PIK3, an enzyme often overexpressed in cancer cells, plays a crucial role in tumor cell regulation and survival. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
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522-17-8 / MFCD01740600
(7As,13As)-9,10-Dimethoxy-3,3-Dimethyl-13,13A-Dihydro-3H-Pyrano[2,3-C:6,5-F’]Dichromen-7(7Ah)-One
(7aS,13aS)-9,10-二甲氧基-3,3-二甲基-13,13a-二氢-3H-吡喃并[2,3-c:6,5-f’]二苯并吡喃--7(7aH)-酮
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中华人民共和国
√
112953-11-4 / MFCD01782559
KRX-0601
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648449-76-7 / MFCD09265247
5-[(2,2-Difluoro-1,3-benzodioxol-5-yl)methylene]-2,4-thiazolidinedione
5-[(2,2-二氟-1,3-苯并二恶茂-5-基)亚甲基]噻唑烷-2,4-二酮
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中华人民共和国
937174-76-0 / MFCD14105605
Gsk 690693
4-[2-(4-氨基-1,2,5-恶二唑-3-基)-1-乙基-7-[(3S)-3-哌啶基甲氧基]-1H-咪唑并[4,5-c]吡啶-4-基]-2-甲基-3-丁炔-2-醇
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中华人民共和国