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| Smiles | C[[email protected]@]12C(N3C=NC4=CC=CC=C34)=CC[[email protected]]1([[email protected]@]5(CC=C6[[email protected]@](C)([[email protected]]5(CC2)[H])CC[[email protected]@H](C6)O)[H])[H] |
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| Synonyms | VN/124-1; Galeterone; VN 124;TOK001;TOK 001; (3S,8R,9S,10R,13S,14S)-17-(1H-benzo[d]imidazol-1-yl)-10,13-dimethyl-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol |
| InChI | InChI=1S/C26H32N2O/c1-25-13-11-18(29)15-17(25)7-8-19-20-9-10-24(26(20,2)14-12-21(19)25)28-16-27-22-5-3-4-6-23(22)28/h3-7,10,16,18-21,29H,8-9,11-15H2,1-2H3/t18-,19-,20-,21-,25-,26-/m0/s1 |
TOK-001 (VN/124-1; Galeterone) is a multifunctional antiandrogen and CYP17 inhibitor(IC50=47 nM) in castration resistant prostate cancer (CRPC). IC50 value: 47 nM Target: CYP17 TOK-001 and abiraterone reduced AR protein and mRNA expression, and antagonized AR-dependent promoter activation induced by androgen.
| Galeterone?(TOK-001?or?VN/124-1) is a novel?antiandrogen?under development by?Tokai Pharmaceuticals?for the treatment of?prostate cancer. It possesses a unique dual?mechanism of action, acting as both anandrogen receptor?antagonist?and an?inhibitor?of?CYP ......by BOC Sciences |
| TOK-001 is a multifunctional antiandrogen and CYP17 inhibitor (IC50=47 nM) in castration resistant prostate cancer (CRPC). ......by MedChemexpress Co., Ltd. |
| Shelf life: >2 years if stored properly Drug formulation: ......by MedKoo Biosciences, Inc. |
| Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2. ......by Selleck Chemicals LLC |
| Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2. ......by Target Molecule Corp. |
| Animal Models | Male severe combined immunodeficient (SCID) mice inoculated subcutaneously (s.c.) with LAPC4 cells |
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| Dosage | 50 mg/kg |
| Formulation | Prepared at 17.2 mg/mL in a 0.3% solution of hydroxypropyl cellulose in saline |
| Administration | Injection s.c. twice daily |
| Source | Selleck Chemicals LLC |
| Appearance:White to off-white solid | EBNumber:EB000028832 |
| DMSO | by MedChemexpress Co., Ltd. |
| (25°C) * In vitro DMSO 24 mg/mL (61.76 mM); Ethanol40 mg/mL warming (102.94 mM); Water<1 mg/mL (<1 mM); In vivo 0.5% hydroxyethyl cellulose30 mg/mL | by Selleck Chemicals LLC |
| Signaling Pathways | Metabolic Enzyme/Protease |
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| Target | Cytochrome P450 |
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| Research Area | Cancer |
|---|
| Indications | Hormone refractory prostate cancer | Hormone refractory prostate cancer |
|---|
| Product Name | Sponsor & Collaborators | Indications | Start Date | End Date | Phase |
|---|---|---|---|---|---|
| TOK-001 | Tokai Pharmaceuticals Inc | Hormone refractory prostate cancer | 2012/12/31 | 2014/9/30 | Phase 2 Clinical |
| TOK-001 | Tokai Pharmaceuticals Inc | Hormone refractory prostate cancer | 2009/10/31 | 2012/8/31 | Phase 1 Clinical |
| TOK-001 | - | Phase 3 |
| Company | Price and Availability | Country/Region |
|---|---|---|
| BOC Sciences | ||
| Biochempartner Co., Ltd | China | |
| CHEMSCENE, LLC | 5mg/USD60();10mg/USD90() | USA |
| MedChemexpress Co., Ltd. | 5mg/USD60();10mg/USD90() | USA |
| MedKoo Biosciences, Inc. | USA | |
| Pure Chemistry Scientific Inc. | 5mg/USDnull(In stock) | USA |
| Selleck Chemicals LLC | 5mg/USD170(In stock);10mM/1mLIn DMSO/USD260(In stock);25mg/USD470(In stock);50mg/USD670(In stock);200mg/USD1670(In stock) | USA |
| Shanghai Haoyuan Chemexpress Co., Ltd. | 5mg/USD60();10mg/USD90() | China |
| Target Molecule Corp. | 5mg/USD97();10mg/USD171();50mg/USD528() | USA |
| Name | CAS No | Formula | MW |
|---|
| Name | CAS No | Formula | MW |
|---|---|---|---|
| Dafadine-A | 1065506-69-5 | C23H25N3O3 | 391.46 |
| VT-464 (racemate) | 1375603-36-3 | C18H17F4N3O3 | 399.34 |
| VT-464 | 1610537-15-9 | C18H17F4N3O3 | 399.34 |
| Isosilybin | 72581-71-6 | C25H22O10 | 482.44 |
| Memantine (hydrochloride) | 41100-52-1 | C12H22ClN | 215.76 |
| Clarithromycin | 81103-11-9 | C38H69NO13 | 747.95 |
| (+)-Ketoconazole | 142128-59-4 | C26H28Cl2N4O4 | 531.43 |
| (+)-Ketoconazole | 142128-59-4 | C26H28Cl2N4O4 | 531.4309 |
| Galangin | 548-83-4 | ||
| Bergapten | 484-20-8 | C12H8O4 | 216.19 |
| Naringin | 10236-47-2 | C27H32O14 | 580.53 |
| Diosmetin | 520-34-3 | C16H12O6 | 300.26 |
| Fenofibrate | 49562-28-9 | C20H21ClO4 | 360.83 |
| Bergaptol | 486-60-2 | C11H6O4 | 202.1629 |
| Talarozole (R enantiomer) | 870093-23-5 | C21H23N5S | 377.5058 |
| Choline Fenofibrate | 856676-23-8 | C22H28ClNO5 | 421.91 |
| Talarozole | 201410-53-9 | C21H23N5S | 377.51 |
| Isavuconazole | 241479-67-4 | C22H17F2N5OS | 437.4650864 |
| Cobicistat | 1004316-88-4 | C40H53N7O5S2 | 776.02 |
| Methoxsalen | 298-81-7 | C12H8O4 | 216.19 |
| Name | CAS No | Formula | MW |
|---|---|---|---|
| TAK-700 (R-form) | 752243-39-3 | C18H17N3O2 | 307.35 |
| Olaparib | 763113-22-0 | C24H23FN4O3 | 434.46 |
| KX2-391 | 897016-82-9 | C26H29N3O3 | 431.53 |
| Bicalutamide | 90357-06-5 | C18H14F4N2O4S | 430.37 |
| Enzalutamide | 915087-33-1 | C21H16F4N4O2S | 464.44 |
| Linsitinib | 867160-71-2 | C26H23N5O | 421.49 |
| Fenretinide | 65646-68-6 | C26H33NO2 | 391.55 |
| Retaspimycin | 857402-23-4 | C31H45N3O8 | 587.7 |
| Retaspimycin (Hydrochloride) | 857402-63-2 | C31H46ClN3O8 | 624.17 |
| Bafetinib | 859212-16-1 | C30H31F3N8O | 576.6154 |
| AT13387 | 912999-49-6 | C24H31N3O3 | 409.52 |
| Tasquinimod | 254964-60-8 | C20H17F3N2O4 | 406.36 |
| Orteronel | 566939-85-3 | C18H17N3O2 | 307.35 |
| Orteronel (racemate) | 426219-18-3 | C18H17N3O2 | 307.3465 |
| TAK-700 (salt) | 426219-53-6 | C28H28N4O7 | 532.54 |
| Cabozantinib | 849217-68-1 | C28H24FN3O5 | 501.51 |
| Odanacatib | 603139-19-1 | C25H27F4N3O3S | 525.56 |
| Zibotentan | 186497-07-4 | C19H16N6O4S | 424.43 |
| Danusertib | 827318-97-8 | C26H30N6O3 | 474.55 |
| Atrasentan | 173937-91-2 | C29H38N2O6 | 510.62 |
