Drug Information

Drug (ID: DG01191) and It's Reported Resistant Information
Name
Cabazitaxel
Synonyms
CABAZITAXEL; 183133-96-2; Jevtana; Taxoid XRP6258; Cabazitaxelum; TXD 258; Xrp6258; XRP-6258; UNII-51F690397J; XRP 6258; Jevtana (TN); CHEBI:63584; NSC-761432; 51F690397J; kabazitaxel; Jevtana Kit; Cabazitaxel (Jevtana); (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-11-hydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate.; cabazitaxel acetonate; Cabazitaxel Injection; Cabazitaxel [USAN:INN]; Jevanta; TXD258; RPR 116258A; RPR-116258A; Cabazitaxel (USAN/INN); SCHEMBL179674; GTPL6798; CHEMBL1201748; AMY4317; DTXSID40171389; EX-A838; TXD-258; C45H57NO14; MFCD18827611; NSC761432; NSC794609; s3022; ZINC85536932; AKOS032947285; CCG-270519; CS-0972; DB06772; NSC 761432; NSC-794609; NCGC00346704-01; NCGC00346704-03; AS-75355; HY-15459; X7252; A25044; D09755; AB01273971-01; AB01273971_02; Q412963; SR-01000941585; J-011721; J-519981; SR-01000941585-1; (((tertbutoxy)carbonyl)amino)-2-hydroxy-3-phenylpropanoate1-hydroxy-7beta,10beta-dimethoxy-9-oxo-5beta,20-epoxytax-11-ene-2alpha,4,13alpha-triyl 4-acetate 2-benzoate 13-((2R,3S)-3-; (1S)-5beta,20-Epoxy-9-oxo-7beta,10beta-dimethoxytaxa-11-ene-1,2alpha,4alpha,13alpha-tetraol 2-benzoate 4-acetate 13-[(2R,3S)-2-hydroxy-3-(tert-butoxycarbonylamino)-3-phenylpropionate]; (1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-(acetyloxy)-15-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-3-phenylpropanoyl]oxy}-1-hydroxy-9,12-dimethoxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0(3),(1) .0 , ]heptadec-13-en-2-yl benzoate; (1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-(acetyloxy)-15-{[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-3-phenylpropanoyl]oxy}-1-hydroxy-9,12-dimethoxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0^{3,10}.0^{4,7}]heptadec-13-en-2-yl benzoate; (2alpha,5beta,7beta,10beta,13alpha)-4-acetoxy-13-({(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate; (2AR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-11-hydroxy-4,6-dimethoxy-4a,8,13,1; (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-9-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-11-hydroxy-4,6-dimethoxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate; [(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; 1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-ene-2,4,13-triyl 4-acetate 2-benzoate 13-((2R,3S)-3-(((tertbutoxy)carbonyl)amino)-2-hydroxy-3-phenylpropanoate); 1-hydroxy-7 ,10 -dimethoxy-9-oxo-5 ,20-epoxytax-11-ene-2 ,4,13 -triyl 4-acetate 2-benzoate 13-[(2R,3S)-3-{[(tert-butoxy)carbonyl]amino}-2-hydroxy-3-phenylpropanoate]; Benzenepropanoic acid, beta-[[(1,1-dimethylethoxy)carbonyl]amino]-alpha-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, (alphaR,betaS)-
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Indication
In total 2 Indication(s)
Breast cancer [ICD-11: 2C60]
Approved
[1]
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Approved
[1]
Structure
Drug Resistance Disease(s)
Disease(s) with Resistance Information Discovered by Cell Line Test for This Drug (1 diseases)
Prostate cancer [ICD-11: 2C82]
[1]
Target Tubulin (TUB) NOUNIPROTAC [1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula
C45H57NO14
IsoSMILES
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
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
InChIKey
BMQGVNUXMIRLCK-OAGWZNDDSA-N
PubChem CID
9854073
ChEBI ID
CHEBI:63584
TTD Drug ID
D02HSB
INTEDE ID
DR0252
DrugBank ID
DB06772
Type(s) of Resistant Mechanism of This Drug
  UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Click to Show/Hide the Resistance Disease of This Class
Prostate cancer [ICD-11: 2C82]
Click to Show/Hide
Drug Resistance Data Categorized by Their Corresponding Mechanisms
       Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Phosphatase and tensin homolog (PTEN) [1]
Molecule Alteration Expression
Down-regulation
 Molecule Info 
Resistant Disease Prostate cancer [ICD-11: 2C82.0]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model CAL27 cells Oral Homo sapiens (Human) CVCL_1107
LOVO cells Colon Homo sapiens (Human) CVCL_0399
BxPC-3 cells Pancreas Homo sapiens (Human) CVCL_0186
C4-2 cells Prostate Homo sapiens (Human) CVCL_4782
HuTu80 cells Small intestine Homo sapiens (Human) CVCL_1301
DU145-DR cells Brain Homo sapiens (Human) CVCL_4Y36
Experiment for
Molecule Alteration		 Western blotting analysis
Experiment for
Drug Resistance		 MTT assay
Mechanism Description TUBB3 expression was upregulated in DTX-resistant and CBZ-resistant cells. TUBB3 knockdown re-sensitized DTX-resistant cells to DTX and CBZ-resistant cells to CBZ. Additionally, TUBB3 knockdown re-sensitized DTX-resistant cell lines to CBZ, indicating that TUBB3 mediates cross-resistance between DTX and CBZ. Knockdown of TUBB3 enhanced PTEN expression, and PTEN knockout enhanced TUBB3 expression.
Key Molecule: Tubulin beta-3 chain (TUBB3) [1]
Molecule Alteration Expression
Up-regulation
 Molecule Info 
Resistant Disease Prostate cancer [ICD-11: 2C82.0]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model CAL27 cells Oral Homo sapiens (Human) CVCL_1107
LOVO cells Colon Homo sapiens (Human) CVCL_0399
BxPC-3 cells Pancreas Homo sapiens (Human) CVCL_0186
C4-2 cells Prostate Homo sapiens (Human) CVCL_4782
HuTu80 cells Small intestine Homo sapiens (Human) CVCL_1301
DU145-DR cells Brain Homo sapiens (Human) CVCL_4Y36
Experiment for
Molecule Alteration		 Western blotting analysis
Experiment for
Drug Resistance		 MTT assay
Mechanism Description TUBB3 expression was upregulated in DTX-resistant and CBZ-resistant cells. TUBB3 knockdown re-sensitized DTX-resistant cells to DTX and CBZ-resistant cells to CBZ. Additionally, TUBB3 knockdown re-sensitized DTX-resistant cell lines to CBZ, indicating that TUBB3 mediates cross-resistance between DTX and CBZ. Knockdown of TUBB3 enhanced PTEN expression, and PTEN knockout enhanced TUBB3 expression.
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Phosphatase and tensin homolog (PTEN) [1]
Molecule Alteration Expression
Up-regulation
 Molecule Info 
Sensitive Disease Prostate cancer [ICD-11: 2C82.0]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model CAL27 cells Oral Homo sapiens (Human) CVCL_1107
LOVO cells Colon Homo sapiens (Human) CVCL_0399
BxPC-3 cells Pancreas Homo sapiens (Human) CVCL_0186
C4-2 cells Prostate Homo sapiens (Human) CVCL_4782
HuTu80 cells Small intestine Homo sapiens (Human) CVCL_1301
DU145-DR cells Brain Homo sapiens (Human) CVCL_4Y36
Experiment for
Molecule Alteration		 Western blotting analysis
Experiment for
Drug Resistance		 MTT assay
Mechanism Description TUBB3 expression was upregulated in DTX-resistant and CBZ-resistant cells. TUBB3 knockdown re-sensitized DTX-resistant cells to DTX and CBZ-resistant cells to CBZ. Additionally, TUBB3 knockdown re-sensitized DTX-resistant cell lines to CBZ, indicating that TUBB3 mediates cross-resistance between DTX and CBZ. Knockdown of TUBB3 enhanced PTEN expression, and PTEN knockout enhanced TUBB3 expression.
Key Molecule: Tubulin beta-3 chain (TUBB3) [1]
Molecule Alteration Expression
Down-regulation
 Molecule Info 
Sensitive Disease Prostate cancer [ICD-11: 2C82.0]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model CAL27 cells Oral Homo sapiens (Human) CVCL_1107
LOVO cells Colon Homo sapiens (Human) CVCL_0399
BxPC-3 cells Pancreas Homo sapiens (Human) CVCL_0186
C4-2 cells Prostate Homo sapiens (Human) CVCL_4782
HuTu80 cells Small intestine Homo sapiens (Human) CVCL_1301
DU145-DR cells Brain Homo sapiens (Human) CVCL_4Y36
Experiment for
Molecule Alteration		 Western blotting analysis
Experiment for
Drug Resistance		 MTT assay
Mechanism Description TUBB3 expression was upregulated in DTX-resistant and CBZ-resistant cells. TUBB3 knockdown re-sensitized DTX-resistant cells to DTX and CBZ-resistant cells to CBZ. Additionally, TUBB3 knockdown re-sensitized DTX-resistant cell lines to CBZ, indicating that TUBB3 mediates cross-resistance between DTX and CBZ. Knockdown of TUBB3 enhanced PTEN expression, and PTEN knockout enhanced TUBB3 expression.
References
Ref 1 TUBB3 Reverses Resistance to Docetaxel and Cabazitaxel in Prostate Cancer .Int J Mol Sci. 2019 Aug 13;20(16):3936. doi: 10.3390/ijms20163936. 10.3390/ijms20163936

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