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Ask your administrator if you think this is wrong. ====== Cabazitaxel 0.001μM R05 exp223 ====== ==== Mechanism of Action ==== Microtubule stabilizer, semi-synthetic taxane * **<color #00a2e8>Class / Subclass 1:</color>** Cell Cycle / Microtubule Poison * **<color #00a2e8>Class / Subclass 2:</color>** Organelle Function / Cytoskeletal Inhibitor ==== Technical Notes ==== <accordion collapsed='true'> <panel title='Compound References' collapsed='true'> * **<color #00a2e8>PubChem Name:</color>** %%Cabazitaxel%% * **<color #00a2e8>Synonyms:</color>** XRP6258; RPR-116258A; taxoid XRP6258 * **<color #00a2e8>CAS #:</color>** 183133-96-2 * **<color #00a2e8>PubChem CID:</color>** [[https://pubchem.ncbi.nlm.nih.gov/compound/9854073|9854073]] * **<color #00a2e8>IUPAC:</color>** %%[(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-acetyloxy-1-hydroxy-15-[(2R,3S)-2-hydroxy-3-[(2-methylpropan-2-yl)oxycarbonylamino]-3-phenylpropanoyl]oxy-9,12-dimethoxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.03,10.04,7]heptadec-13-en-2-yl] benzoate%% * **<color #00a2e8>INCHI Name:</color>** InChI=1S/C45H57NO14/c1-24-28(57-39(51)33(48)32(26-17-13-11-14-18-26)46-40(52)60-41(3,4)5)22-45(53)37(58-38(50)27-19-15-12-16-20-27)35-43(8,36(49)34(55-10)31(24)42(45,6)7)29(54-9)21-30-44(35,23-56-30)59-25(2)47/h11-20,28-30,32-35,37,48,53H,21-23H2,1-10H3,(H,46,52)/t28-,29-,30+,32-,33+,34+,35-,37-,43+,44-,45+/m0/s1 * **<color #00a2e8>INCHI Key:</color>** BMQGVNUXMIRLCK-OAGWZNDDSA-N * **<color #00a2e8>Molecular Weight:</color>** 835.9 * **<color #00a2e8>Canonical SMILES:</color>** CC1=C2C(C(=O)C3(C(CC4C(C3C(C(C2(C)C)(CC1OC(=O)C(C(C5=CC=CC=C5)NC(=O)OC(C)(C)C)O)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)OC)C)OC * **<color #00a2e8>Isomeric SMILES:</color>** CC1=C2[C@H](C(=O)[C@@]3([C@H](C[C@@H]4[C@]([C@H]3[C@@H]([C@@](C2(C)C)(C[C@@H]1OC(=O)[C@@H]([C@H](C5=CC=CC=C5)NC(=O)OC(C)(C)C)O)O)OC(=O)C6=CC=CC=C6)(CO4)OC(=O)C)OC)C)OC * **<color #00a2e8>Molecular Formula:</color>** C45H57NO14 {{:chemogenomics:structures:chem-0128.svg?nolink}} </panel> <panel title='Compound Supplier' collapsed='true'> * **<color #00a2e8>Supplier Name:</color>** APExBIO * **<color #00a2e8>Catalog #:</color>** B2157 * **<color #00a2e8>Lot #:</color>** N/A </panel> <panel title='Compound Characterization' collapsed='true'> * **<color #00a2e8>HRMS (ESI-TOF) m/z:</color>** (M+H)+ Calcd for C45H57NO14 836.38518; found 836.38653 </panel> <panel title='Dose Response Curve' collapsed='true'> * **<color #00a2e8>Platform ID:</color>** Cabazitaxel * **<color #00a2e8>Min:</color>** 10.7396; **<color #00a2e8>Max:</color>** 88.0253 {{:chemogenomics:dose_response:dr_193.png?nolink&500 |}} \\ \\ \\ \\ |< 300px 100px 200px >| ^ IC ^ Concentration (µM) ^ | IC10 |N/A | | IC20 |0.0006 | | IC30 |0.0008 | | IC40 |0.0011 | | IC50 |0.0015 | | IC60 |N/A | | IC70 |N/A | | IC80 |N/A | | IC90 |N/A | \\ </panel> </accordion> ==== Screen Summary ==== * **<color #00a2e8>Round</color>**: 05 * **<color #00a2e8>Dose</color>**: 1nM * **<color #00a2e8>Days of incubation</color>**: 8 * **<color #00a2e8>Doublings</color>**: 6.5 * **<color #00a2e8>Numbers of reads</color>**: 22466532 ==== Screen Results ==== ^Sensitive/Resistant hits (FDR<0.05)^CRANKS^Score Plot^Top 30 Genes^Screen Similarity^Top 30 Sensitive GO terms^Top 30 Resistant GO terms^ |20/1|<color #e85500>[[https://files.tyerslab.com/files/public/chemogenomics/cranks/Cabazitaxel_0.001uM_Round-5_exp223.txt|Scores]]</color>|<button type="primary" size="sm" modal="ScorePlot">View</button>|<button type="primary" size="sm" modal="modal_hits">View</button>|<button type="primary" size="sm" modal="modal_screen_similarity">View</button>|<button type="primary" size="sm" modal="modal_go_sensitive">View</button>|<button type="default" size="sm" modal="modal_go_resistant">View</button>| <modal id='ScorePlot' size='lg' title='Cabazitaxel 0.001μM R05 exp223'> {{:chemogenomics:cranks_plots:exp223.png?nolink}} </modal> <modal id="modal_hits" size="sm" title="Top 30 S/R Genes"> ^Gene^CRANKS Score^FDR^ |[[:human_genes:K:KATNA1|KATNA1]]|-4.75|<0.01| |[[:human_genes:K:KIF2A|KIF2A]]|-4.04|<0.01| |[[:human_genes:W:WDR62|WDR62]]|-3.68|<0.01| |[[:human_genes:K:KATNB1|KATNB1]]|-3.66|<0.01| |[[:human_genes:G:GNA13|GNA13]]|-3.47|<0.01| |[[:human_genes:C:CEP170|CEP170]]|-2.80|<0.01| |[[:human_genes:K:KATNBL1|KATNBL1]]|-2.78|<0.01| |[[:human_genes:K:KIF18B|KIF18B]]|-2.78|<0.01| |[[:human_genes:A:ASPM|ASPM]]|-2.77|0.02| |[[:human_genes:D:DLGAP5|DLGAP5]]|-2.77|<0.01| |[[:human_genes:P:PCBP2|PCBP2]]|-2.74|<0.01| |[[:human_genes:D:DEPDC5|DEPDC5]]|-2.69|0.01| |[[:human_genes:R:RHOA|RHOA]]|-2.63|0.01| |[[:human_genes:I:ITPK1|ITPK1]]|-2.55|0.02| |[[:human_genes:B:BUB1B|BUB1B]]|-2.55|0.04| |[[:human_genes:T:TACC3|TACC3]]|-2.50|0.02| |[[:human_genes:C:CCDC69|CCDC69]]|-2.49|0.02| |[[:human_genes:M:MSI2|MSI2]]|-2.47|0.02| |[[:human_genes:D:DPAGT1|DPAGT1]]|-2.44|0.06| |[[:human_genes:D:DDX39A|DDX39A]]|-2.38|0.04| |[[:human_genes:Q:QRICH1|QRICH1]]|-2.35|0.13| |[[:human_genes:S:SCAPER|SCAPER]]|-2.34|0.05| |[[:human_genes:C:CDSN|CDSN]]|-2.32|0.09| |[[:human_genes:R:RIC8A|RIC8A]]|-2.31|0.05| |[[:human_genes:M:MAPKAP1|MAPKAP1]]|-2.29|0.06| |[[:human_genes:R:RSRC2|RSRC2]]|-2.23|0.41| |[[:human_genes:A:ATP2B1|ATP2B1]]|-2.21|0.13| |[[:human_genes:S:SNF8|SNF8]]|-2.21|0.13| |[[:human_genes:F:FAM60A|FAM60A]]|-2.20|0.09| |[[:human_genes:A:ADAD2|ADAD2]]|-2.20|0.09| |[[:human_genes:R:RBM38|RBM38]]|1.93|0.41| |[[:human_genes:K:KLHL18|KLHL18]]|1.94|0.41| |[[:human_genes:P:PLN|PLN]]|1.96|0.72| |[[:human_genes:A:ARHGEF35|ARHGEF35]]|1.98|0.57| |[[:human_genes:S:SPP1|SPP1]]|1.99|0.35| |[[:human_genes:H:HK2|HK2]]|2.00|0.70| |[[:human_genes:R:RASAL1|RASAL1]]|2.00|0.35| |[[:human_genes:L:LYSMD2|LYSMD2]]|2.02|0.34| |[[:human_genes:R:RRP9|RRP9]]|2.05|0.31| |[[:human_genes:C:CETN3|CETN3]]|2.05|0.31| |[[:human_genes:P:PSMD1|PSMD1]]|2.07|0.54| |[[:human_genes:S:SLC22A17|SLC22A17]]|2.07|0.31| |[[:human_genes:B:B3GALT6|B3GALT6]]|2.07|0.39| |[[:human_genes:K:KCNK17|KCNK17]]|2.10|0.35| |[[:human_genes:S:SOGA1|SOGA1]]|2.11|0.35| |[[:human_genes:D:DUSP5|DUSP5]]|2.13|0.26| |[[:human_genes:E:EPG5|EPG5]]|2.15|0.26| |[[:human_genes:C:C5orf51|C5orf51]]|2.18|0.31| |[[:human_genes:U:USP9X|USP9X]]|2.18|0.26| |[[:human_genes:A:AHCYL1|AHCYL1]]|2.20|0.31| |[[:human_genes:C:CDK13|CDK13]]|2.27|0.26| |[[:human_genes:A:AK2|AK2]]|2.29|0.26| |[[:human_genes:M:MAPKAPK5|MAPKAPK5]]|2.30|0.26| |[[:human_genes:S:SMARCC1|SMARCC1]]|2.31|0.26| |[[:human_genes:P:PSG11|PSG11]]|2.37|0.26| |[[:human_genes:P:PNPLA6|PNPLA6]]|2.43|0.26| |[[:human_genes:G:GOLGA6L6|GOLGA6L6]]|2.48|0.26| |[[:human_genes:T:TAF1|TAF1]]|2.68|0.26| |[[:human_genes:N:NDUFA12|NDUFA12]]|2.74|0.14| |[[:human_genes:C:CLASP1|CLASP1]]|4.26|<0.01| </modal> <modal id="modal_screen_similarity" size="lg" title="Correlated Screens"> ^Screen^Correlation^Plot^ |[[:results:exp231|Epothilone-B 0.0015μM R05 exp231]]|0.152|<button type="primary" size="small" modal="1">View</button>| |[[:results:exp184|Ixabepilone 0.004 to 0.005μM on day4 R04 exp184]]|0.141|<button type="primary" size="small" modal="2">View</button>| |[[:results:exp103|Taxol 0.004μM R03 exp103]]|0.096|<button type="primary" size="small" modal="3">View</button>| |[[:results:exp159|Docetaxel 0.001 to 0.002μM on day4 R04 exp159]]|0.092|<button type="primary" size="small" modal="4">View</button>| |[[:results:exp45|Docetaxel 0.002μM R01 exp45]]|0.089|<button type="primary" size="small" modal="5">View</button>| |[[:results:exp232|Epothilone-D 0.004 to 0.006μM on day4 R05 exp232]]|0.086|<button type="primary" size="small" modal="6">View</button>| |[[:results:exp243|S-trityl-L-cysteine 0.5μM R05 exp243]]|0.076|<button type="primary" size="small" modal="7">View</button>| |[[:results:exp179|Combretastatin A4 0.002 to 0.003μM day4 R04 exp179]]|0.058|<button type="primary" size="small" modal="8">View</button>| |[[:results:exp190|Vincristine 0.0005μM R04 exp190]]|0.057|<button type="primary" size="small" modal="9">View</button>| |[[:results:exp107|UMK57 0.6μM R03 exp107]]|0.053|<button type="primary" size="small" modal="10">View</button>| |[[:results:exp310|2-Methoxyestradiol 0.55μM R07 exp310]]|0.062|<button type="primary" size="small" modal="11">View</button>| </modal> <modal id="1" size="lg" title="Cabazitaxel 0.001μM R05 exp223 vs Epothilone-B 0.0015μM R05 exp231"> {{:chemogenomics:comparison_plots:exp223_vs_exp231.png?nolink |}} </modal> <modal id="2" size="lg" title="Cabazitaxel 0.001μM R05 exp223 vs Ixabepilone 0.004 to 0.005μM on day4 R04 exp184"> {{:chemogenomics:comparison_plots:exp184_vs_exp223.png?nolink |}} </modal> <modal id="3" size="lg" title="Cabazitaxel 0.001μM R05 exp223 vs Taxol 0.004μM R03 exp103"> {{:chemogenomics:comparison_plots:exp103_vs_exp223.png?nolink |}} </modal> <modal id="4" size="lg" title="Cabazitaxel 0.001μM R05 exp223 vs Docetaxel 0.001 to 0.002μM on day4 R04 exp159"> {{:chemogenomics:comparison_plots:exp159_vs_exp223.png?nolink |}} </modal> <modal id="5" size="lg" title="Cabazitaxel 0.001μM R05 exp223 vs Docetaxel 0.002μM R01 exp45"> {{:chemogenomics:comparison_plots:exp223_vs_exp45.png?nolink |}} </modal> <modal id="6" size="lg" title="Cabazitaxel 0.001μM R05 exp223 vs Epothilone-D 0.004 to 0.006μM on day4 R05 exp232"> {{:chemogenomics:comparison_plots:exp223_vs_exp232.png?nolink |}} </modal> <modal id="7" size="lg" title="Cabazitaxel 0.001μM R05 exp223 vs S-trityl-L-cysteine 0.5μM R05 exp243"> {{:chemogenomics:comparison_plots:exp223_vs_exp243.png?nolink |}} </modal> <modal id="8" size="lg" title="Cabazitaxel 0.001μM R05 exp223 vs Combretastatin A4 0.002 to 0.003μM day4 R04 exp179"> {{:chemogenomics:comparison_plots:exp179_vs_exp223.png?nolink |}} </modal> <modal id="9" size="lg" title="Cabazitaxel 0.001μM R05 exp223 vs Vincristine 0.0005μM R04 exp190"> {{:chemogenomics:comparison_plots:exp190_vs_exp223.png?nolink |}} </modal> <modal id="10" size="lg" title="Cabazitaxel 0.001μM R05 exp223 vs UMK57 0.6μM R03 exp107"> {{:chemogenomics:comparison_plots:exp107_vs_exp223.png?nolink |}} </modal> <modal id="11" size="lg" title="2-Methoxyestradiol 0.55μM R07 exp310 vs Cabazitaxel 0.001μM R05 exp223"> {{:chemogenomics:comparison_plots:exp223_vs_exp310.png?nolink |}} </modal> <modal id="modal_go_sensitive" size="lg" title="Top 30 sensitive GO terms"> ^GO Term^Fold Change^Genes^ |katanin complex|443.84|KATNA1,KATNB1,KATNBL1| |cytoplasmic microtubule organization|40.81|KATNA1,KATNB1,KATNBL1,RHOA| |mitotic spindle organization|31.15|KIF2A,WDR62,DLGAP5,RHOA,TACC3| |spindle pole|27.85|KATNA1,KIF2A,WDR62,KATNB1,KATNBL1,ASPM,DLGAP5,TACC3| |spindle organization|24.08|KIF2A,WDR62,ASPM,DLGAP5,RHOA,TACC3,CCDC69| |mitotic spindle|23.40|KATNA1,WDR62,KATNBL1,KIF18B,ASPM,DLGAP5,TACC3| |microtubule cytoskeleton organization involved in mitosis|22.94|KIF2A,WDR62,DLGAP5,RHOA,TACC3| |midbody|18.21|KATNA1,KATNB1,KATNBL1,ASPM,RHOA,CCDC69| |spindle|17.15|KATNA1,KIF2A,WDR62,KATNB1,CEP170,KATNBL1,KIF18B,ASPM,DLGAP5,BUB1B,TACC3,CCDC69| |nuclear chromosome segregation|16.21|KIF2A,KATNB1,KIF18B,ASPM,DLGAP5,RHOA| |microtubule binding|15.63|KATNA1,KIF2A,KATNB1,KATNBL1,KIF18B,DLGAP5,CCDC69| |chromosome segregation|12.67|KIF2A,KATNB1,KIF18B,ASPM,DLGAP5,RHOA,CCDC69| |microtubule cytoskeleton organization|12.08|KATNA1,KIF2A,WDR62,KATNB1,KATNBL1,KIF18B,ASPM,DLGAP5,RHOA,TACC3,CCDC69| |tubulin binding|11.32|KATNA1,KIF2A,KATNB1,KATNBL1,KIF18B,DLGAP5,CCDC69| |cell division|9.36|KATNA1,KIF2A,KATNB1,KIF18B,ASPM,RHOA,BUB1B,TACC3| |mitotic cell cycle process|9.14|KIF2A,WDR62,KATNB1,KIF18B,DLGAP5,RHOA,BUB1B,TACC3| |microtubule-based process|8.35|KATNA1,KIF2A,WDR62,KATNB1,KATNBL1,KIF18B,ASPM,DLGAP5,RHOA,TACC3,CCDC69| |microtubule organizing center|7.34|KATNA1,KIF2A,WDR62,KATNB1,CEP170,KATNBL1,ASPM,DLGAP5,BUB1B,TACC3| |cell cycle process|6.77|KIF2A,WDR62,KATNB1,KIF18B,ASPM,DLGAP5,RHOA,BUB1B,TACC3,CCDC69| </modal> <modal id="modal_go_resistant" size="lg" title="Top 30 resistant GO terms">No GO term hits below threshold. (FDR <0.05)</modal> Last modified: 2026/01/15 21:36by 127.0.0.1