Bcl-2

下级目录

SK1-I

ABT-199

DAT-230

Apoptone

(3'R,6S,9R)-5,6,7,8,9,10-Hexahydro-5'-(2,2,2-trifluoroethyl)-2-[(1E)-3-[4-(trifluoromethyl)-1-piperidinyl]-1-propen-1-yl]spiro[6,9-methanobenzocyclooctene-11,3'-[1,2,5]thiadiazolidine]1',1'-dioxide

Avanbulin

YC-137

RO-3306

Supinoxin

IG-105

PaloMid529(P529)

GSK1059615

HA14-1

Bisindolylmaleimide IX (mesylate)

Paclitaxel

Triciribine

Roscovitine

CHLORIN E6

Atiprimod (free base)

Ortataxel

生根粉263

Tosedostat

N-[4-(2-叔丁基苯磺酰基)苯基]-2,3,4-三羟基-5-(2-异丙基苄基)苯甲酰胺

目录项下的产品

1025065-69-3 / MFCD125065693
SGI-1776
N-[(1-甲基-4-哌啶基)甲基]-3-[3-(三氟甲氧基)苯基]-咪唑并[1,2-b]哒嗪-6-胺

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
试剂

中华人民共和国

1072443-89-0 / MFCD172443890
BML-258 HCl was removed and discontinued.
SK1-I

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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1235859-13-8 / MFCD335859138
Nanatinostat, also known as Tractinostat, CHR-3996 and VRx-3996, is an orally bioavailable, second-generation hydroxamic acid-based inhibitor of histone deacetylase (HDAC) with potential antineoplastic activity. HDAC inhibitor CHR-3996 inhibits HDAC, resulting in an accumulation of highly acetylated histones, the induction of chromatin remodeling, and the selective transcription of tumor suppressor genes; these events may result in the inhibition of tumor cell division and the induction of tumor cell apoptosis. This agent may upregulate HSP70 and downregulate anti-apoptotic Bcl-2 proteins more substantially than some first-generation HDAC inhibitors. HDACs, upregulated in many tumor cell types, are a family of metalloenzymes responsible for the deacetylation of chromatin histone proteins.

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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1257044-40-8 / MFCD357044408
2-((7H-Pyrrolo[2,3-b]pyridin-5-yl)oxy)-4-(4-((4'-chloro-5,5-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((3-nitro-4-(((tetrahydro-2H-pyran-4-yl)methyl)amino)phenyl)sulfonyl)benzamide
2-((7H-吡咯并[2,3-b]吡啶-5-基)氧基)-4-(4-((4'-氯-5,5-二甲基-3,4,5,6-四氢-[1,1'-联苯]-2-基)甲基)哌嗪-1-基)-N-(3-硝基-4-(((四氢-2H-吡喃-4-基)甲基氨基)苯基)磺酰基)苯甲酰胺

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
试剂

中华人民共和国
√

1504583-00-9 / MFCD604583009
DAT-230 is a promising microtubule inhibitor that has great potential for the treatment of fibrosarcoma in vitro and in vivo. DAT-230 exhibited potent anti-proliferative activity against various cancer cells. DAT-230 -treatment in HT-1080 cells resulted in microtubule de-polymerization and G2/M phase arrest preceding apoptosis. Phosphor-cdc2 (thr14/tyr15) reduction, cyclin B1 accumulation and aberrant spindles denoted the cyclin B1-cdc2 complex active and M phase arrest in HT-1080 cells treated with DAT-230. Apoptosis induced by DAT-230 was related with the activation of caspase-9, caspase-3 and PARP cleavage, which were at the downstream of mitochondria.

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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183387-50-0 / MFCD83387500
Apoptone, also known as HE3235, is an orally bioavailable adrenal steroid analogue with potential antineoplastic activity. Androstane steroid HE3235 appears to bind the androgen receptor (AR), down-regulating anti-apoptotic genes, such as Bcl-2, while increasing the expression of pro-apoptotic genes, such as caspases. In vitro and in vivo studies indicate that this agent inhibits androstenediol-dependent LNCaP cell tumor growth. In addition, HE3235 may potentiate chemotherapeutic agents by down-regulating ABCG2, the gene encoding the multi-drug resistant (MDR) protein MDR2.

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199796-52-6 / MFCD99796526
DHA-paclitaxel, also know as Taxoprexin, is prodrug comprised of the naturally occurring omega-3 fatty acid docosahexaenoic acid (DHA) covalently conjugated to the anti-microtubule agent paclitaxel. Because tumor cells take up DHA, DHA-paclitaxel is delivered directly to tumor tissue, where the paclitaxel moiety binds to tubulin and inhibits the disassembly of microtubules, thereby resulting in the inhibition of cell division. Paclitaxel also induces apoptosis by binding to and blocking the function of the apoptosis inhibitor protein Bcl-2 (B-cell Leukemia 2). DHA-paclitaxel exhibits improved pharmacokinetic and toxicity profiles when compared to conventional paclitaxel and has demonstrated antineoplastic activity in animal models of cancer.

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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623165-93-5 / MFCD23165935
MRK003 is a γ-secretase inhibitor exhibits promising in vitro pre-clinical activity in multiple myeloma and non-Hodgkin's lymphoma. MRK003 treatment induced caspase-dependent apoptosis and inhibited proliferation of MM and NHL cell lines and patient cells. Examination of signaling events after treatment showed time-dependent decrease in levels of the notch intracellular domain, Hes1 and c-Myc. MRK003 downregulated cyclin D1, Bcl-Xl and Xiap levels in NHL cells and p21, Bcl-2 and Bcl-Xl in MM cells. In addition, MRK003 caused an upregulation of pAkt, indicating crosstalk with the PI3K/Akt pathway.
(3'R,6S,9R)-5,6,7,8,9,10-六氢-5'-(2,2,2-三氟乙基)-2-[(1E)-3-[4-(三氟甲基)-1-哌啶基]-1-丙烯-1-基]螺[6,9-亚甲基苯并环辛烯E-11,3'-[1,2,5]噻二唑烷]1',1'-二氧化物

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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798577-91-0 / MFCD98577910
Avanbulin, also known as BAL27862, is a novel synthetic potent inhibitor of tubulin polymerization that induces cancer cell death. BAL27862 is a novel microtubule-destabilizing drug that is currently undergoing phase I clinical evaluation as the prodrug BAL101553. BAL27862 elicits a unique microtubule (MT) phenotype, distinct from paclitaxel, vinblastine and colchicine, has broad in vitro anti-proliferative activity against a diverse range of human tumor lines (low nM IC50s) and induces significant antitumor responses in a range.

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810659-53-1 / MFCD10659531
YC-137 is a BCL-2 inhibitor, which selectively induces apoptosis of Bcl-2-overexpressing cells and disrupts its interaction with Bid BH3, thereby blocking the anti-apoptotic activity of Bcl-2.

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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872573-93-8 / MFCD72573938
RO-3306
2-[[(噻吩-2-基)甲基]氨基]-5-[1-(喹啉-6-基)甲-(Z)-亚基]噻唑-4-酮

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
试剂

中华人民共和国

888478-45-3 / MFCD88478453
Supinoxin

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
试剂

905978-63-4 / MFCD005978634
IG-105 is a potent microtubule inhibitor with potential anticancer activity. IG-105 inhibits microtubule assembly by binding at colchicine pocket. IG-105 shows a potent anticancer activity in vitro and in vivo and has good safety in mice. IG-105 showed a potent activity against human leukemia and solid tumors in breast, liver, prostate, lung, skin, colon, and pancreas with IC(50) values between 0.012 and 0.298 mumol/L. It was also active in drug-resistant tumor cells and not a P-glycoprotein substrate. It inhibited microtubule assembly followed by M-phase arrest, Bcl-2 inactivation, and then apoptosis through caspase pathways.

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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914913-88-5 / MFCD014913885
8-(1-Hydroxyethyl)-2-Methoxy-3-((4-Methoxybenzyl)Oxy)-6H-Benzo[c]Chromen-6-One
8-(1-羟乙基)-2-甲氧基-3-((4-甲氧基苄基)氧基)-6H-苯并[c]苯并吡喃-6-酮

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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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).

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
试剂

65673-63-4 / MFCD00218213
HA14-1
乙基-2-氨基-6-溴-4-(1-氰基-2-乙氧基-2-甲酰)-4H-苯并呋喃-3-羧酸

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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中华人民共和国
北京市
√

138489-18-6 / MFCD00236436
3-{1-[3-(Amidinothio)Propyl]-3-Indolyl}-4-(1-Methyl-3-Indolyl)-1H-Pyrrole-2,5-Dione Methanesulfonate
3-(3-(4-(1-甲基-1H-吲哚-3-基)-2,5-二氧代-2,5-二氢-1H-吡咯-3-基)-1H-吲哚-1-基)丙基异硫脲甲磺酸盐

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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33069-62-4 / MFCD00869953
Paclitaxel
紫杉醇

原料 0 #^资源 0.0^询 0.0^%成交 ^交易量
试剂

中华人民共和国
北京市
√
山东省

35943-35-2 / MFCD00932413
(2R,3R,4S,5R)-2-(3-Amino-5-Methyl-1,4,5,6,8-Pentaazaacenaphthylen-1(5H)-Yl)-5-(Hydroxymethyl)Tetrahydrofuran-3,4-Diol
(2R,3R,4S,5R)-2-(3-氨基-5-甲基-1,4,5,6,8-五氮杂苊烯-1(5H)-基)-5-(羟甲基)四氢呋喃-3,4-二醇

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
试剂

中华人民共和国
√

186692-46-6 / MFCD02266401
Roscovitine
(R)-2-((6-(苄基氨基)-9-异丙基-9H-嘌呤-2-基)氨基)丁-1-醇

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
试剂

中华人民共和国
√

19660-77-6 / MFCD07364062
Chlorin E6
二氢卟吩E6

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
试剂

123018-47-3 / MFCD09837657
Atiprimod is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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186348-23-2 / MFCD09837792
Ortataxel, also known as IDN5109, is novel seimsynthetic taxane with potential anticancer activity. Ortataxel is characterized by its high tolerability, antitumor efficacy, ability to overcome multidrug resistance, and oral bioavailabilty. In in vitro experiments, IDN5109 showed antiproliferative effects against HNSCC cell lines. After treatment with IDN5109, Bcl-2 and Bcl-XL were down-regulated, Bax was up-regulated, and caspase-3 was activated. After treatment with IDN5109, concentrations of both VEGF and IL-8 in the culture supernatant of HNSCC cells decreased. In in vivo experiments, the oral administration of IDN5109 showed antitumor effects against HNSCC tumor xenografts. Immunohistochemistry showed that IDN5109 inhibited tumor angiogenesis and induced apoptosis in HNSCC cells, producing a decreased blood vessel density and increased apoptosis index. On the basis of these results, IDN5109 is useful as a chemotherapeutic agent against HNSCC.

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923564-51-6 / MFCD12756219
(R)-4-(4-((4’-Chloro-4,4-Dimethyl-3,4,5,6-Tetrahydro-[1,1’-Biphenyl]-2-Yl)Methyl)Piperazin-1-Yl)-N-((4-((4-Morpholino-1-(Phenylthio)Butan-2-Yl)Amino)-3-((Trifluoromethyl)Sulfonyl)Phenyl)Sulfonyl)Benzamide
(R)-4-(4-((4’-氯-4,4-二甲基-3,4,5,6-四氢-[1,1’-联苯]-2-基)甲基)哌嗪-1-基)-N-((4-((4-吗啉-1-(苯硫基)丁烷-2-基)氨基)-3-((三氟甲基)磺酰)苯基)磺酰)苯甲酰胺

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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238750-77-1 / MFCD13185162
Tosedostat
托舍多特

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
试剂

中华人民共和国

877877-35-5 / MFCD17010275
TW-37 is a small-molecule inhibitor of Bcl-2 family proteins, inhibited cell growth and induced apoptosis in pancreatic cancer. TW-37 induces cell growth inhibition and S-phase cell cycle arrest, with regulation of several important cell cycle-related genes like p27, p57, E2F-1, cdc25A, CDK4, cyclin A, cyclin D1, and cyclin E. The cell growth inhibition was accompanied by increased apoptosis with concomitant attenuation of Notch-1, Jagged-1, and its downstream genes such as Hes-1 in vitro and in vivo.
N-[4-(2-叔丁基苯磺酰基)苯基]-2,3,4-三羟基-5-(2-异丙基苄基)苯甲酰胺

原料 0 ^资源 0.0^询 0.0^%成交 ^交易量
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