BAY 87-2243
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MedKoo CAT#: 205901

CAS#: 1227158-85-1

Description: BAY 87-2243 is a highly potent and selective inhibitor of hypoxia-induced gene activation, which has antitumor activities by inhibition of mitochondrial complex I. BAY 87-2243 mproves local tumor control after fractionated irradiation in a schedule-dependent manner in head and neck human xenografts. BAY-87-2243 markedly decreased nuclear HIF-1α expression and pimonidazole hypoxic fraction already after 3 days of drug treatment. BAY-87-2243 prior to RT significantly reduced TCD50 from 123 to 100 Gy (p=0.037). Additional BAY-87-2243 application during RT did not decrease TCD50.


Price and Availability

Size
Price

2mg
USD 70
10mg
USD 250
100mg
USD 1250
1g
USD 3250
Size
Price

3mg
USD 90
25mg
USD 450
200mg
USD 1950
2g
USD 4650
Size
Price

5mg
USD 150
50mg
USD 750
500mg
USD 2450
5g
Ask price

BAY 87-2243, purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 205901
Name: BAY 87-2243
CAS#: 1227158-85-1
Chemical Formula: C26H26F3N7O2
Exact Mass: 525.21
Molecular Weight: 525.54
Elemental Analysis: C, 59.42; H, 4.99; F, 10.85; N, 18.66; O, 6.09


Synonym: BAY 872243; BAY872243; BAY-872243.

IUPAC/Chemical Name: 1-cyclopropyl-4-[4-[[5-methyl-3-[3-[4-(trifluoromethoxy)phenyl]-1,2,4-oxadiazol-5-yl]-1H-pyrazol-1-yl]methyl]-2-pyridinyl]-piperazine

InChi Key: CDJNNOJINJAXPV-UHFFFAOYSA-N

InChi Code: InChI=1S/C26H26F3N7O2/c1-17-14-22(25-31-24(33-38-25)19-2-6-21(7-3-19)37-26(27,28)29)32-36(17)16-18-8-9-30-23(15-18)35-12-10-34(11-13-35)20-4-5-20/h2-3,6-9,14-15,20H,4-5,10-13,16H2,1H3

SMILES Code: FC(F)(F)OC1=CC=C(C2=NOC(C3=NN(CC4=CC(N5CCN(C6CC6)CC5)=NC=C4)C(C)=C3)=N2)C=C1


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>5 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
293490


Additional Information

  
 
 
 


References

1: Chang E, Liu H, Unterschemmann K, Ellinghaus P, Liu S, Gekeler V, Cheng Z, Berndorff D, Gambhir SS. 18F-FAZA PET imaging response tracks the reoxygenation of tumors in mice upon treatment with the mitochondrial complex I inhibitor BAY 87-2243. Clin Cancer Res. 2015 Jan 15;21(2):335-46. doi: 10.1158/1078-0432.CCR-14-0217. Epub 2014 Nov 7. PubMed PMID: 25381339; PubMed Central PMCID: PMC4297600.

2: Helbig L, Koi L, Brüchner K, Gurtner K, Hess-Stumpp H, Unterschemmann K, Baumann M, Zips D, Yaromina A. BAY 87-2243, a novel inhibitor of hypoxia-induced gene activation, improves local tumor control after fractionated irradiation in a schedule-dependent manner in head and neck human xenografts. Radiat Oncol. 2014 Sep 19;9:207. doi: 10.1186/1748-717X-9-207. PubMed PMID: 25234922; PubMed Central PMCID: PMC4262387.

3: Ellinghaus P, Heisler I, Unterschemmann K, Haerter M, Beck H, Greschat S, Ehrmann A, Summer H, Flamme I, Oehme F, Thierauch K, Michels M, Hess-Stumpp H, Ziegelbauer K. BAY 87-2243, a highly potent and selective inhibitor of hypoxia-induced gene activation has antitumor activities by inhibition of mitochondrial complex I. Cancer Med. 2013 Oct;2(5):611-24. doi: 10.1002/cam4.112. Epub 2013 Aug 20. PubMed PMID: 24403227; PubMed Central PMCID: PMC3892793.