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DMXAA (Synonyms: ASA-404; Vadimezan)

Cat. No.: HY-10964 Purity: 99.19%
Data Sheet SDS Handling Instructions

DMXAA is a competitive inhibitor of the enzyme DT-diaphorase (NAD(P)H:Quinone oxidoreductase EC 1.6.99.2) with respect to NADH, with Ki values of 20 μM.

For research use only. We do not sell to patients.
DMXAA Chemical Structure

DMXAA Chemical Structure

CAS No. : 117570-53-3

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10 mM * 1 mL in DMSO $88 In-stock
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50 mg $440 In-stock
100 mg $700 In-stock
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  • Biological Activity

  • Protocol

  • Technical Information

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  • References

Description

DMXAA is a competitive inhibitor of the enzyme DT-diaphorase (NAD(P)H:Quinone oxidoreductase EC 1.6.99.2) with respect to NADH, with Ki values of 20 μM. [1] IC50 value: 20 μM (Ki) [1] Target: DT-diaphorase in vitro: DMXAA partially inhibits cytochrome b5 reductase activity. [1] DMXAA is a potent tumor blood vessel-disrupting agent and cytokine inducer used for the treatment of non-small cell lung cancer (NSCLC) and other cancers. DMXAA significantly induces G1 phase arrest in A549 cells. DMXAA induces apoptosis via a mitochondria-dependent pathway and promoted autophagy, as indicated by the increased level of cytosolic cytochrome c, activation of caspase 3, and enhances expression of beclin 1 and microtubule-associated protein 1A/1B-light chain 3 (LC3-II) in A549 cells. [2] in vivo: DMXAA has been shown to potentiate the antitumour activity of several bioreductive drugs in vivo. [1] In contrast, treatment with DMXAA results in a significant lower amount in the tumours when compared to the control mice.[3]

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00863733 Cancer Research UK|Cancer Society Auckland Solid Tumors May 1996 Phase 1
NCT00856336 Antisoma Research Refractory Tumors May 2003 Phase 1
NCT00832494 Antisoma Research Non-Small Cell Lung Cancer September 2004 Phase 1|Phase 2
NCT01290380 Novartis Pharmaceuticals|Novartis Solid Tumor Malignancies February 2010 Phase 1
NCT01278758 Novartis Pharmaceuticals|Novartis Metastatic Cancer March 2010 Phase 1
NCT00111618 Antisoma Research Prostate Cancer May 2005 Phase 2
NCT01299415 Novartis Pharmaceuticals|Novartis Solid Tumors August 2009 Phase 1
NCT01285453 Novartis Pharmaceuticals|Novartis Advanced or Recurrent Solid Tumors March 2009 Phase 1
NCT00003697 University of Glasgow|National Cancer Institute (NCI) Unspecified Adult Solid Tumor, Protocol Specific October 1995 Phase 1
NCT01057342 Swiss Group for Clinical Cancer Research Lung Cancer January 2010 Phase 2
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References
Molecular Weight

282.29

Formula

C₁₇H₁₄O₄

CAS No.

117570-53-3

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 6.5 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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DMXAA
Cat. No.:
HY-10964
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