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1610537-15-9 (VT-464)

1

Identification

VT-464 VT-464
Name VT-464
Formula C18H17F4N3O3
MW 399.34
CAS No. 1610537-15-9
EINECS
Smiles FC(F)OC1=C(OC(F)F)C=C(C=CC([[email protected]](C2=CNN=N2)(C(C)C)O)=C3)C3=C1
Synonyms VT464;VT 464; (S)-1-(6,7-bis(difluoromethoxy)naphthalen-2-yl)-2-methyl-1-(1H-1,2,3-triazol-4-yl)propan-1-ol
InChI InChI=1S/C18H17F4N3O3/c1-9(2)18(26,15-8-23-25-24-15)12-4-3-10-6-13(27-16(19)20)14(28-17(21)22)7-11(10)5-12/h3-9,16-17,26H,1-2H3,(H,23,24,25)/t18-/m0/s1
2

Introduction

VT-464 is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition. IC50 value: 69 nM(h-CYP17 Lyase) [1] Target: CYP17 Lyase inhibitor in vitro: VT-464, a non-steroidal small molecule inhibits androgen production without mineralocorticoid excess or cortisol depletion by selective inhibition of CYP17 17,20-lyase.

Background Information

VT-464 is a potent CYP17 lyase inhibitor(h-Lyase IC50=69 nM) that demonstrated both exceptional in vitro lyase/hydroxylase selectivity (~10-fold) and oral activity in a hamster model of androgen biosynthesis inhibition. IC50 value: 69 nM(h-CYP17 Lyase) [1] Target: CYP17 Lyase inhibitor in vitro: VT-464, a non-steroidal small molecule inhibits androgen production without mineralocorticoid excess or cortisol depletion by selective inhibition of CYP17 17,20-lyase. We determined the impact of VT-464 on tumor growth of a mCRPC xenograft, MDA-PCa-133, in vivo, and on androgen signaling in C4-2B prostate cancer cells in vitro [2]. in vivo: The MDA-PCa-133 xenograft is derived from a clinical CRPC bone metastasis. Subcutaneous MDA-PCa-133 tumor expresses PSA, full-length androgen receptor (AR) and AR-V7 isoform. We determined the effect of VT464 and AA on MDA-PCa-133 growing in tumor-bearing castrated male mice: randomization into three groups; oral treatment with vehicle only, VT-464, (100 mg/kg bid), or AA (100 mg/kg bid) for 25 days. Both VT-464 and AA reduced tumor volume (>two fold compared to vehicle; p<0.05). These results indicate that selective VT-464 CYP17 lyase inhibition is as effective as AA CYP17 inhibition in this model [2]. ......by MedChemexpress Co., Ltd.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

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Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000010874

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
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Mechanism and Indication

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Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
VT-464 Viamet Pharmaceuticals, Inc. Prostate Cancer 2014/4/22 Phase 2 Clinical
VT-464 Viamet Pharmaceuticals, Inc. Castration-resistant Prostate Cancer 2013/12/6 Phase 2 Clinical
VT-464 - Phase 2
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Safety Data of VT-464

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Spectral Information

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Suppliers List

Company Price and Availability Country/Region
Apexbio Technology LLC 5mg/USD332();10mg/USD475();50mg/USD1425();100mg/USD1995() USA
CHEMSCENE, LLC USA
MedChemexpress Co., Ltd. 5mg/USD350(In stock);10mg/USD500(In stock);50mg/USD1500(In stock);100mg/USD2100(In stock) USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD350(Get quote);10mg/USD500(Get quote);50mg/USD1500(Get quote);100mg/USD2100(Get quote) China
10

Related Products

Other Forms of 1610537-15-9

Name CAS No Formula MW
VT-464 (racemate) 1375603-36-3 C18H17F4N3O3 399.34
VT-464 (R enantiomer) 1375603-38-5 C18H17F4N3O3 399.34

Recommended Compounds in Cytochrome P450

Name CAS No Formula MW
Dafadine-A 1065506-69-5 C23H25N3O3 391.46
VT-464 (racemate) 1375603-36-3 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 65277-42-1 C26H28Cl2N4O4 531.43
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
4-hydroxy-7H-furo[3,2-g]chromen-7-one 486-60-2 C11H6O4 202.16
(R)-Talarozole 870093-23-5 C21H23N5S 377.51
Choline Fenofibrate 856676-23-8 C22H28ClNO5 421.91
Talarozole 201410-53-9 C21H23N5S 377.51
BAL 4815 241479-67-4 C22H17F2N5OS 437.47
Cobicistat 1004316-88-4 C40H53N7O5S2 776.02
Methoxsalen 298-81-7 C12H8O4 216.19
TAK-700 (R-form) 752243-39-3 C18H17N3O2 307.35

Recommended Compounds in Same Indication

Name CAS No Formula MW
Degarelix 214766-78-6 C82H103ClN18O16 1632.26
Vadimezan? 117570-53-3 C17H14O4 282.29
Satraplatin 129580-63-8 C10H22Cl2N2O4Pt 500.28
ODM-201 1297538-32-9 C19H19ClN6O2 398.85
Pexidartinib 1029044-16-3 C20H15ClF3N5 417.81
AZD3965 1448671-31-5 C21H24F3N5O5S 515.51
VT-464 (racemate) 1375603-36-3 C18H17F4N3O3 399.34
Dolastatin 10 110417-88-4 C42H68N6O6S 785.09
Leucylarginylproline 133943-59-6 C17H32N6O4 384.47
S-methyl-KE-298 143584-75-2 C13H16O3S 252.33
Lycopene 502-65-8 C40H56 536.87
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Route of Synthesis

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References

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More Information

VT-464

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