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Medical Research Areas
Cytosketetal Signaling
Microtubule
Microtubule
下级目录
ARQ621
AZD4877
MPT0B214
ELR510444
MPT0B098
HAC-Y6
DAT-230
HMN-176
Cabazitaxel
DHA-paclitaxel
ER-67880
Milataxel
E7974
Avanbulin
ENMD-119
FLUORAPACIN
4SC-207
KX02 (KX2-361)
IG-105
IRC-083927
Epofolate
甲基-(5-[2 - 噻吩羰基]-1H-苯并咪唑-2-基)氨基甲酸酯
2-Methoxyestradiol
Carbendazim
KRIBB3
AVE-8063
IXABEPILONE
Erastin
目录项下的产品
1095253-39-6 / MFCD195253396
ARQ-621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Over-expression of Eg5 causes genomic instability and tumor formation in mice; therefore, Eg5 is a potential anti-cancer target. Preclinical data shows anti-tumor activity of ARQ 621 across a wide range of cell lines from human solid and hematological malignancies.
ARQ621
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0.0
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试剂
1176760-49-8 / MFCD276760498
AZD4877
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0
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0.0
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0.0
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1215208-65-3 / MFCD315208653
MPT0B214 is a novel and potent microtubule inhibitor with potential anticancer activity. MPT0B214 inhibited tubulin polymerization through strongly binding to the tubulin's colchicine-binding site and had cytotoxic activity in a variety of human tumor cell lines. After treatment with MPT0B214, KB cells were arrested in the G2-M phase before cell death occurred, which were associated with upregulation of cyclin B1, dephosphorylation of Cdc2, phosphorylation of Cdc25C and elevated expression of the mitotic marker MPM-2. Furthermore, the compound induced apoptotic cell death through mitochondria/caspase 9-dependent pathway. Notably, several KB-derived multidrug-resistant cancer cell lines were also sensitive to MPT0B214 treatment. ( PLoS One. 2013;8(3):e58953).
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0
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0.0
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0.0
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1233948-35-0 / MFCD333948350
N-(5-(5-Cyanothiophen-2-Yl)-2-Methylphenyl)-4-Methylbenzenesulfonamide
N-(5-(5-氰基噻吩-2-基)-2-甲基苯基)-4-甲基苯磺酰胺
原料
0
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0.0
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0.0
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1254363-89-7 / MFCD354363897
MPT0B098
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0
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0.0
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0.0
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1331959-78-4 / MFCD431959784
HAC-Y6
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0
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0.0
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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.
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0
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0.0
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173529-10-7 / MFCD73529107
(E)-4-(2-((4-Methoxyphenyl)sulfonamido)styryl)pyridine 1-oxide
(E)-4-(2-((4-甲氧基苯基)磺酰胺)苯乙烯基)吡啶 1-氧化物
原料
0
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中华人民共和国
183133-96-2 / MFCD83133962
Benzenepropanoic acid, β-[[(1,1-dimethylethoxy)carbonyl]amino]-α-hydroxy-, (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-11-hydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-yl ester, (αR,βS)-
β-[[(1,1-二甲基乙氧基)羰基]氨基]-α-羟基-苯丙酸,(乙酰氧基)-12-(苯甲酰氧基)- 十二氢-11-羟基-4,6-二甲氧基-4,8,8,13,13-四甲基-5-氧代-7,11-亚甲基-1H-环癸烷[3,4]苯并[1,2-b]氧杂-9-基酯
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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
√
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.
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247186-96-5 / MFCD47186965
ER-67880 is a novel and potent microtubule inhibitor with potential anticancer activity.
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0
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393101-41-2 / MFCD93101412
Milataxel
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0
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0.0
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610787-07-0 / MFCD10787070
E7974 is an analog of the sponge-derived anti-microtubule tripeptide hemiasterlin with antimitotic and potential antineoplastic activities. Hemiasterlin analog E7974 binds to the Vinca domain on tubulin, resulting in inhibition of tubulin polymerization and microtubule assembly; depolymerization of exsiting microtubules; inhibition of mitosis; and inhibition of cellular proliferation. This agent may have more affinity for the beta-3 tubulin isotype. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
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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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864668-87-1 / MFCD64668871
ENMD-119
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0.0
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0.0
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869811-23-4 / MFCD69811234
Bis[(4-fluorophenyl)methyl] trisulfide
二[(4-氟苯基)甲基]三硫化物
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
871015-11-1 / MFCD71015111
4SC-207 is a novel microtubule inhibitor , which shows strong anti-proliferative activity in a large panel of tumor cell lines with an average GI50 of 11 nM. In particular, 4SC-207 is active in multi-drug resistant cell lines, such as HCT-15 and ACHN, suggesting that it is a poor substrate for drug efflux pumps. 4SC-207 inhibits microtubule growth in vitro and in vivo and promotes, in a dose dependent manner, a mitotic delay/arrest, followed by apoptosis or aberrant divisions due to chromosome alignment defects and formation of multi-polar spindles. Furthermore, preliminary data from preclinical studies suggest low propensity towards bone marrow toxicities at concentrations that inhibit tumor growth in paclitaxel-resistant xenograft models. 4SC-207 may be a potential anti-cancer agent.
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0
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897016-26-1 / MFCD97016261
KX02 (KX2-361)
-(3-氟苄基)-2-(5-(4-吗啉代苯基)吡啶-2-基)乙酰胺
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0
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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.
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0
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955082-09-4 / MFCD055082094
IRC-083927 is novel and potent microtubule inhibitor with potential anticancer activity. IRC-083927 inhibits the tubulin polymerization by a binding to the colchicine site. IRC-083927 inhibits in vitro cell growth of human cancer cell lines in the low nanomolar range. More interesting, it remains highly active against cell lines resistant to microtubule-interacting agents (taxanes, Vinca alkaloids, or epothilones). Chronic oral treatment with IRC-083927 (5 mg/kg) inhibits the growth of two human tumor xenografts in nude mice (C33-A, human cervical cancer and MDA-MB-231, human hormone-independent breast cancer). Together, the antitumor effects induced by IRC-083927 on tumor models resistant to tubulin agents support further investigations to fully evaluate its potential for the treatment of advanced cancers, particularly those resistant to current clinically available drugs.
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958646-17-8 / MFCD058646178
Epofolate is folate receptor-targeting antimitotic agent with potential antineoplastic activity. Folate receptor-targeted epothilone BMS753493 contains an epothilone moiety linked to a single folate molecule. Mediated through the folate moiety, this agent delivers the antimitotic epothilone component into cells expressing folic acid receptors, frequently upregulated in many types of tumor cells. After ligand-receptor internalization, the epothilone moiety induces microtubule polymerization and stabilizes microtubules against depolymerization, resulting in the inhibition of mitosis and cellular proliferation. Check for active clinical trials or closed clinical trials using this agent. (NCI Thesaurus).
原料
0
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31430-18-9 / MFCD00005588
Nocodazole
诺考达唑
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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
√
362-07-2 / MFCD00010489
2-Methoxyestradiol
2-甲氧基雌二醇
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
北京市
√
10605-21-7 / MFCD00055390
Methyl 1H-benzo[d]imidazol-2-ylcarbamate
2-(甲氧羰氨基)苯并咪唑
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0
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0.0
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中华人民共和国
北京市
√
129414-88-6 / MFCD00710140
KRIBB3
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0
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162705-07-9 / MFCD00937446
(Z)-2-Methoxy-5-(3,4,5-Trimethoxystyryl)Aniline
(Z)-2-甲氧基-5-(3,4,5-三甲氧基苯乙烯)苯胺
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219989-84-1 / MFCD04307791
Ixabepilone
(1S,3S,7S,10R,11S,12S,16R)-7,11-二羟基-8,8,10,12,16-五甲基-3-((E)-1-(2-甲基噻唑-4-基)丙烷-1-烯-2-基)-17-氧杂-4-氮杂双环并[14.1.0]十七烷-5,9-二酮
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0
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0.0
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0.0
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571203-78-6 / MFCD09837984
2-[1-[4-[2-(4-Chlorophenoxy)acetyl]-1-piperazinyl]ethyl]-3-(2-ethoxyphenyl)-4(3H)-quinazolinone
2-[1-[4-[2-(4-氯苯氧基)乙酰基]-1-哌嗪基]乙基]-3-(2-乙氧基苯基)-4-(3H)-喹唑啉酮
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中华人民共和国
北京市