WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: 125881
CAS#: 685847-78-3 (free base)
Description: PX-478 is an orally active small molecule that inhibits hypoxia-inducible factor 1-alpha (HIF1A) expression, potentially leading to decreased expression of genes important for tumor growth, reduced tumor cell proliferation, and induced apoptosis. Its mechanism of action is independent of VHL and p53 tumor suppressor genes and may involve glucose uptake and metabolism disruption through Glut-1 inhibition. PX-478 demonstrates excellent activity against human tumor xenografts, resulting in tumor regressions and growth delays correlated with HIF-1 levels.
Hodoodo Cat#: 125881
Name: PX-478 free base
CAS#: 685847-78-3 (free base)
Chemical Formula: C13H18Cl2N2O3
Exact Mass: 320.07
Molecular Weight: 321.198
Elemental Analysis: C, 48.61; H, 5.65; Cl, 22.07; N, 8.72; O, 14.94
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Related CAS #: 685898-44-6 (HCl) 685847-78-3 (free base)
Synonym: PX 478; PX-478; PX 478; PX478 free base;
IUPAC/Chemical Name: (S)-4-(2-amino-2-carboxyethyl)-N,N-bis(2-chloroethyl)aniline oxide
InChi Key: GSKQMLGAUOTSKT-LBPRGKRZSA-N
InChi Code: InChI=1S/C13H18Cl2N2O3/c14-5-7-17(20,8-6-15)11-3-1-10(2-4-11)9-12(16)13(18)19/h1-4,12H,5-9,16H2,(H,18,19)/t12-/m0/s1
SMILES Code: N[C@@H](CC1=CC=C(C=C1)[N+]([O-])(CCCl)CCCl)C(O)=O
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
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: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 321.20 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: Lee K, Kim HM. A novel approach to cancer therapy using PX-478 as a HIF-1α inhibitor. Arch Pharm Res. 2011 Oct;34(10):1583-5. doi: 10.1007/s12272-011-1021-3. Review. PubMed PMID: 22076756.
2: Schwartz DL, Bankson JA, Lemos R Jr, Lai SY, Thittai AK, He Y, Hostetter G, Demeure MJ, Von Hoff DD, Powis G. Radiosensitization and stromal imaging response correlates for the HIF-1 inhibitor PX-478 given with or without chemotherapy in pancreatic cancer. Mol Cancer Ther. 2010 Jul;9(7):2057-67. doi: 10.1158/1535-7163.MCT-09-0768. Epub 2010 Jun 29. PubMed PMID: 20587661; PubMed Central PMCID: PMC2935253.
3: Jacoby JJ, Erez B, Korshunova MV, Williams RR, Furutani K, Takahashi O, Kirkpatrick L, Lippman SM, Powis G, O'Reilly MS, Herbst RS. Treatment with HIF-1alpha antagonist PX-478 inhibits progression and spread of orthotopic human small cell lung cancer and lung adenocarcinoma in mice. J Thorac Oncol. 2010 Jul;5(7):940-9. doi: 10.1097/JTO.0b013e3181dc211f. PubMed PMID: 20512076; PubMed Central PMCID: PMC3782111.
4: Schwartz DL, Powis G, Thitai-Kumar A, He Y, Bankson J, Williams R, Lemos R, Oh J, Volgin A, Soghomonyan S, Nishii R, Alauddin M, Mukhopadhay U, Peng Z, Bornmann W, Gelovani J. The selective hypoxia inducible factor-1 inhibitor PX-478 provides in vivo radiosensitization through tumor stromal effects. Mol Cancer Ther. 2009 Apr;8(4):947-58. doi: 10.1158/1535-7163.MCT-08-0981. PubMed PMID: 19372568; PubMed Central PMCID: PMC2908257.
5: Palayoor ST, Mitchell JB, Cerna D, Degraff W, John-Aryankalayil M, Coleman CN. PX-478, an inhibitor of hypoxia-inducible factor-1alpha, enhances radiosensitivity of prostate carcinoma cells. Int J Cancer. 2008 Nov 15;123(10):2430-7. doi: 10.1002/ijc.23807. PubMed PMID: 18729192.
6: Koh MY, Spivak-Kroizman T, Venturini S, Welsh S, Williams RR, Kirkpatrick DL, Powis G. Molecular mechanisms for the activity of PX-478, an antitumor inhibitor of the hypoxia-inducible factor-1alpha. Mol Cancer Ther. 2008 Jan;7(1):90-100. doi: 10.1158/1535-7163.MCT-07-0463. PubMed PMID: 18202012.
7: Jordan BF, Black K, Robey IF, Runquist M, Powis G, Gillies RJ. Metabolite changes in HT-29 xenograft tumors following HIF-1alpha inhibition with PX-478 as studied by MR spectroscopy in vivo and ex vivo. NMR Biomed. 2005 Nov;18(7):430-9. PubMed PMID: 16206237.
8: Jordan BF, Runquist M, Raghunand N, Baker A, Williams R, Kirkpatrick L, Powis G, Gillies RJ. Dynamic contrast-enhanced and diffusion MRI show rapid and dramatic changes in tumor microenvironment in response to inhibition of HIF-1alpha using PX-478. Neoplasia. 2005 May;7(5):475-85. PubMed PMID: 15967100; PubMed Central PMCID: PMC1501160.
9: Welsh S, Williams R, Kirkpatrick L, Paine-Murrieta G, Powis G. Antitumor activity and pharmacodynamic properties of PX-478, an inhibitor of hypoxia-inducible factor-1alpha. Mol Cancer Ther. 2004 Mar;3(3):233-44. PubMed PMID: 15026543.
