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141400-58-0 (PX-12)

1

Identification

PX-12 PX-12
Name PX-12
Formula C7H12N2S2
MW 188.31
CAS No. 141400-58-0
EINECS
Smiles CCC(SSC1=NC=CN1)C
Synonyms PX12;PX 12;IV-2; 2-(sec-butyldisulfanyl)-1H-imidazole
InChI InChI=1S/C7H12N2S2/c1-3-6(2)10-11-7-8-4-5-9-7/h4-6H,3H2,1-2H3,(H,8,9)
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Introduction

PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1(Trx-1) currently in clinical development as an antitumor agent; IC50=7 uM in Hela, MTT assay, 72 h. IC50 value: 7 uM (Hela,72 h, MTT) [1] Target: Thioredoxin-1 in vitro: Based on MTT assays, PX-12 inhibited the growth of HeLa cells with an IC50 value of ~7 μM at 72 h.

Background Information

PX-12 is an irreversible inhibitor of Trx-1 currently in clinical development as an antitumor agent. The research results suggest that the lowering of elevated levels of plasma Trx-1 in cancer patients may provide a surrogate for the inhibition of tumor T ......by BOC Sciences
PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1(Trx-1) currently in clinical development as an antitumor agent; IC50=7 uM in Hela, MTT assay, 72 h. IC50 value: 7 uM (Hela,72 h, MTT) [1] Target: Thioredoxin-1 in vitro: Based on MTT assays, PX-12 inhibited the growth of HeLa cells with an IC50 value of ~7 μM at 72 h. DNA flow cytometry analysis indicated that 5 and 10 μM PX-12 significantly induced a G2/M phase arrest of the cell cycle. PX-12 also increased the number of dead cells and annexin V-fluorescein isothiocyanate-positive cells [1]. in vivo: PX-12 treatment significantly lowered plasma Trx-1 in cancer patients having the highest plasma Trx-1 pretreatment levels. PX-12 treatment also significantly lowered plasma VEGF levels in cancer patients with high pretreatment VEGF levels. SELDI-TOF mass spectrometry identified seven additional plasma proteins whose levels decreased after PX-12 administration, one of which was identified as a truncated form of transthyretin [2]. At the 300 mg/m(2) dose level, one patient experienced a reversible episode of pneumonitis during the first cycle, and a second patient developed pneumonitis after the second cycle. Doses up to 226 mg/m(2) were well tolerated, and grade 3/4 events were uncommon (<3% of patients) [3]. ......by MedChemexpress Co., Ltd.
Shelf life: >2 years if stored properly Drug formulation: ......by MedKoo Biosciences, Inc.
PX-12(IV-2) is an irreversible inhibitor of Thioredoxin-1(Trx-1) currently in clinical development as an antitumor agent; IC50=7 uM in Hela, MTT assay, 72 h. ......by Target Molecule Corp.
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Protocol(Only for Reference)

Cell Experiment

Animal Experiment

4

Physical and Chemical Properties

Appearance:White to off-white Solid EBNumber:EB000015627

Storage condition

Solubility

DMSO by MedChemexpress Co., Ltd.
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Mechanism and Indication

Signaling Pathways Others
Target Others
Research Area Cancer
Indications Pancreatic Neoplasms Metastatic Cancer; Advanced Cancer
6

Clinical Information

Product Name Sponsor & Collaborators Indications Start Date End Date Phase
PX-12 Oncothyreon Inc.; National Cancer Institute (NCI); Translational Genomics Research Institute, Phoenix, Arizona. Pancreatic Neoplasms 2006/12/1 2009/4/1 Phase 2 Clinical
PX-12 Oncothyreon Inc. Metastatic Cancer; Advanced Cancer 2008/6/1 2009/8/1 Phase 1 Clinical
PX-12 - Phase 2
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Safety Data of PX-12

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Spectral Information

9

Suppliers List

Company Price and Availability Country/Region
AdooQ BioScience, LLC 10mg/USD85() USA
Apexbio Technology LLC 10mg/USD123(In stock) USA
BOC Sciences
BioVision, Inc., 5mg/USD115() USA
CHEMSCENE, LLC USA
Cayman Chemical Company 1mg/USD35() USA
MedChemexpress Co., Ltd. 5mg/USD70(In stock);10mg/USD92(In stock);50mg/USD352(In stock);100mg/USD550(In stock);200mg/USD850(In stock) USA
MedKoo Biosciences, Inc. USA
Santa Cruz Biotechnology, Inc. 10mg/USD115() USA
Selleck Chemicals LLC USA
Shanghai Haoyuan Chemexpress Co., Ltd. 5mg/USD70(In stock);10mg/USD92(In stock);50mg/USD352(In stock) China
Sigma-Aldrich, Inc. 5mg/USD106() USA
Target Molecule Corp. 10mg/USD80();50mg/USD291() USA
Tocris Bioscience Inc. 10mg/USD119() USA
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Related Products

Other Forms of 141400-58-0

Name CAS No Formula MW

Recommended Compounds in Others

Name CAS No Formula MW
(R)-(+)-Etomoxir (sodium salt) 828934-41-4 C15H18ClNaO4 320.74
Dictamine 484-29-7 C12H9NO2 199.21
Liothyronine (sodium) 55-06-1 C15H11I3NNaO4 672.96
Afobazole (hydrochloride) 173352-39-1 C15H22ClN3O2S 343.87
FPH2 957485-64-2 C14H16ClN5O2S 353.83
α-Tocopherol (phosphate) 38976-17-9 C29H51O5P 510.69
BAMB-4 891025-25-5 C15H12N2O2 252.27
LDN-27219 312946-37-5 C20H16N4O2S2 408.5
ISO-1 478336-92-4 C12H13NO4 235.24
Aurothioglucose 12192-57-3 C6H11AuO5S 392.18
Oxybenzone 131-57-7 C14H12O3 228.24
ITX3 347323-96-0 C22H17N3OS 371.45
Cardiogreen 3599-32-4 C43H47N2NaO6S2 774.96
Skp2 Inhibitor C1 432001-69-9 C18H13BrN2O4S2 465.34
INH1 313553-47-8 C18H16N2OS 308.4
PF6-AM 1268491-69-5 C33H31BO12 630.4
XEN445 1515856-92-4 C18H17F3N2O3 366.33
Methyl N-ethyl-N-4-(5-nitro-2,1-benzisothiazol-3-yl)azophenyl-alaninate 52239-04-0 C19H19N5O4S 413.45
1,4-bis(Butylamino)anthraquinone 17354-14-2 C22H26N2O2 350.45
CID 797718 370586-05-3 C12H11NO3 217.22

Recommended Compounds in Same Indication

Name CAS No Formula MW
Imexon 59643-91-3 C4H5N3O 111.1
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Route of Synthesis

12

References

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More Information

PX-12

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