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Apaziquone

  CAS No.: 141304-51-0   Cat No.: BADC-00593 4.5  

Apaziquone is an indolequinone bioreductive prodrug and analog of mitomycin C with potential antineoplastic and radiosensitization activities. Apaziquone is converted to active metabolites in hypoxic cells by intracellular reductases, which are present in greater amounts in hypoxic tumor cells. The active metabolites alkylate DNA, resulting in apoptotic cell death.

Apaziquone

Structure of 141304-51-0

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Category
ADC Cytotoxin
Molecular Formula
C15H18O3
Molecular Weight
246.3
Shipping
Room temperature

* For research and manufacturing use only. We do not sell to patients.

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Synonyms
1H-INDOLE-4,7-DIONE, 5-(1-AZIRIDINYL)-3-(HYDROXYMETHYL)-2-(3-HYDROXY-1-PROPENYL)-1-METHYL-, (E)-; APAZIQUONE
IUPAC Name
5-(aziridin-1-yl)-3-(hydroxymethyl)-2-[(E)-3-hydroxyprop-1-enyl]-1-methylindole-4,7-dione
Canonical SMILES
CN1C(=C(C2=C1C(=O)C=C(C2=O)N3CC3)CO)C=CCO
InChI
InChI=1S/C15H16N2O4/c1-16-10(3-2-6-18)9(8-19)13-14(16)12(20)7-11(15(13)21)17-4-5-17/h2-3,7,18-19H,4-6,8H2,1H3/b3-2+
InChIKey
MXPOCMVWFLDDLZ-NSCUHMNNSA-N
Shipping
Room temperature
In Vitro
Apaziquone treatment inhibited cell proliferation and induced apoptosis in OSCC cells in vitro. Apaziquone treated OSCC cells showed increased activation of Caspase 9 and Caspase 3, and Poly (ADP ribose) polymerase (PARP) cleavage suggesting induction of apoptosis by apaziquone in oral cancer cells. Importantly, apaziquone treatment significantly reduced oral tumor xenograft volume in immunocompromised NOD/SCID/Crl mice without causing apparent toxicity to normal tissues.
In Vivo
Intravesical administration of 4 mg/40 ml apaziquone was well tolerated and had ablative activity against superficial bladder cancer marker lesions. Haematuria can reduce the potency of apaziquone in this experimental model. These findings impact upon the design of further phase III clinical trials and strongly suggest that apaziquone should not be administered immediately after transurethral resection of non-muscle invasive bladder cancer when haematuria is common.
NCT NumberCondition Or DiseasePhaseStart DateSponsorStatus
NCT01469221Bladder CancerPhase 32017-12-15Spectrum Pharmaceuticals, IncTerminated (Business reason)
NCT00141531Bladder NeoplasmsPhase 22012-06-14Spectrum Pharmaceuticals, IncCompleted
NCT00461591Bladder CancerPhase 32021-03-30Spectrum Pharmaceuticals, IncCompleted
NCT02563561Bladder CancerPhase 32021-10-27Spectrum Pharmaceuticals, IncTerminated
NCT03224182Bladder CancerPhase 32021-09-28Spectrum Pharmaceuticals, IncTerminated (Suspended development)

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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