Home Other Building Blocks 918633-87-1
918633-87-1,MFCD22420822
Catalog No.:AA00GU4A

918633-87-1 | Th-302

Pack Size
Purity
Availability
Price(USD)
Quantity
  
2mg
98%
in stock  
$27.00   $19.00
- +
5mg
98%
in stock  
$46.00   $32.00
- +
10mg
98%
in stock  
$68.00   $48.00
- +
25mg
98%
in stock  
$113.00   $79.00
- +
250mg
97%
in stock  
$795.00   $557.00
- +
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
  • Request for Quotation
  • Download SDS
  • Technical Information
  • Properties
  • Downstream Synthesis Route
  • Literature
Technical Information
Catalog Number:
AA00GU4A
Chemical Name:
Th-302
CAS Number:
918633-87-1
Molecular Formula:
C9H16Br2N5O4P
Molecular Weight:
449.0362
MDL Number:
MFCD22420822
SMILES:
BrCCNP(=O)(NCCBr)OCc1cnc(n1C)[N+](=O)[O-]
Properties
Computed Properties
 
Complexity:
374  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
21  
Hydrogen Bond Acceptor Count:
7  
Hydrogen Bond Donor Count:
2  
Rotatable Bond Count:
9  
XLogP3:
0.6  

Downstream Synthesis Route
141025-16-3    39070-14-9   
N,N’-bis(2-bromoethyl)phosphorodiamidicacid(1-methyl-2-nitro-1H-imidazol-5-yl)methylester 

[1]JournalofMedicinalChemistry,2008,vol.51,p.2412-2420

[2]Patent:WO2016/11195,2016,A1.Locationinpatent:Paragraph0053;0103

[1]CurrentPatentAssignee:IMMUNOGENESISINC-WO2016/11195,2016,A1

C4H10Br2ClN2OP 
  39070-14-9   
N,N’-bis(2-bromoethyl)phosphorodiamidicacid(1-methyl-2-nitro-1H-imidazol-5-yl)methylester 

[1]ACSMedicinalChemistryLetters,2017,vol.8,p.1269-1274

2576-47-8    39070-14-9   
N,N’-bis(2-bromoethyl)phosphorodiamidicacid(1-methyl-2-nitro-1H-imidazol-5-yl)methylester 

[1]Patent:CN110746459,2020,A.Locationinpatent:Paragraph0039;0056-0061

Literature

Title: Randomized Phase II Trial of Gemcitabine Plus TH-302 Versus Gemcitabine in Patients With Advanced Pancreatic Cancer.

Journal: Journal of clinical oncology : official journal of the American Society of Clinical Oncology 20150501

Title: Metabolism and excretion of TH-302 in dogs.

Journal: Xenobiotica; the fate of foreign compounds in biological systems 20120701

Title: TH-302, a hypoxia-activated prodrug with broad in vivo preclinical combination therapy efficacy: optimization of dosing regimens and schedules.

Journal: Cancer chemotherapy and pharmacology 20120601

Title: Metabolism, pharmacokinetics and excretion of a novel hypoxia activated cytotoxic prodrug, TH-302, in rats.

Journal: Xenobiotica; the fate of foreign compounds in biological systems 20120401

Title: Pharmacokinetics of TH-302: a hypoxically activated prodrug of bromo-isophosphoramide mustard in mice, rats, dogs and monkeys.

Journal: Cancer chemotherapy and pharmacology 20120301

Title: Molecular and cellular pharmacology of the hypoxia-activated prodrug TH-302.

Journal: Molecular cancer therapeutics 20120301

Title: Selective tumor hypoxia targeting by hypoxia-activated prodrug TH-302 inhibits tumor growth in preclinical models of cancer.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20120201

Title: Phase 1 study of the safety, tolerability, and pharmacokinetics of TH-302, a hypoxia-activated prodrug, in patients with advanced solid malignancies.

Journal: Clinical cancer research : an official journal of the American Association for Cancer Research 20110501

Title: Targeting the multiple myeloma hypoxic niche with TH-302, a hypoxia-activated prodrug.

Journal: Blood 20100902

Title: Inhibition of both thioredoxin reductase and glutathione reductase may contribute to the anticancer mechanism of TH-302.

Journal: Biological trace element research 20100901

Title: Potent and highly selective hypoxia-activated achiral phosphoramidate mustards as anticancer drugs.

Journal: Journal of medicinal chemistry 20080424

Title: Meng F, et al. Enhancement of hypoxia-activated prodrug TH-302 anti-tumor activity by Chk1 inhibition. BMC Cancer. 2015 May 21;15:422.

Title: Zhang X, et al. MR Imaging Biomarkers to Monitor Early Response to Hypoxia-Activated Prodrug TH-302 in Pancreatic Cancer Xenografts. PLoS One. 2016 May 26;11(5):e0155289.

Title: Peeters SG, et al. TH-302 in Combination with Radiotherapy Enhances the Therapeutic Outcome and Is Associated with Pretreatment 8FHX4 Hypoxia PET Imaging. Clin Cancer Res. 2015 Jul 1;21(13):2984-92.

Quotation Request
Company Name:
*
Contact Person:
*
Email:
*
Quantity Required:
*
Country:
Additional Info:
SDS
Related Products of 918633-87-1
Tags:918633-87-1 Molecular Formula|918633-87-1 MDL|918633-87-1 SMILES|918633-87-1 Th-302