Motexafin lutetium hydrate
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 201942

CAS#: 156436-90-7

Description: Motexafin lutetium is a texaphyrin, marketed as Antrin by Pharmacyclics Inc. Motexafin lutetium is structurally a pentadentate aromatic metallotexaphyrin with photosensitizing properties. Motexafin lutetium preferentially accumulates in tumor cells due to their increased rates of metabolism and absorbs light, forming an extended high energy conformational state that produces high quantum yields of singlet oxygen, resulting in local cytotoxic effects. M otexafin lutetium is a photosensitiser for use in photodynamic therapy to treat skin conditions and superficial cancers. It has also been tested for use in photoangioplasty (photodynamic treatment of diseased arteries). It is photoactivated by 732 nm light which allows greater depth of penetration.


Chemical Structure

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Motexafin lutetium hydrate
CAS# 156436-90-7

Theoretical Analysis

MedKoo Cat#: 201942
Name: Motexafin lutetium hydrate
CAS#: 156436-90-7
Chemical Formula: C52H74LuN5O15
Exact Mass:
Molecular Weight: 1166.12
Elemental Analysis: C, 53.56; H, 6.22; Lu, 15.00; N, 6.01; O, 19.21

Size Price Shipping out time Quantity
1mg USD 250 Same Day
2mg USD 450 Same Day
5mg USD 750 Same Day
10mg USD 1250 Same Day
25mg USD 2150 Same Day
50mg USD 3650 Same Day
100mg USD 5950 Same Day
Inquire bulk and customized quantity

Pricing updated 2021-03-09. Prices are subject to change without notice.

Motexafin lutetium hydrate, purity > 98%, is in stock. The same day shipping out after order is received.

Synonym: PCI-0123; PCI 0123; PCI0123; Lu texaphyrin; LuTex; Lutetium texaphyrin; Lutrin; Optrin; Brand name: Antrin. Pubchem: CID 9919942

IUPAC/Chemical Name: Lutetium, bis(acetato-κO)[9,10-diethyl-20,21-bis[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]-4,15-dimethyl-8,11-imino-3,6:16,13-dinitrilo-1,18-benzodiazacycloeicosine-5,14-dipropanolato-κN1,κN18,κN23,κN24,κN25]-, hydrate, (PB-7-11-233'2'4)- [Note: this is the name used in sci-finder]

InChi Key: NHCMWCKTFZJXSD-RPQFQESVSA-L

InChi Code: InChI=1S/C48H66N5O10.2C2H4O2.Lu/c1-7-35-36(8-2)40-28-42-38(12-10-14-55)34(4)46(53-42)32-50-44-30-48(63-26-24-61-22-20-59-18-16-57-6)47(62-25-23-60-21-19-58-17-15-56-5)29-43(44)49-31-45-33(3)37(11-9-13-54)41(52-45)27-39(35)51-40;2*1-2(3)4;/h27-32,54-55H,7-26H2,1-6H3;2*1H3,(H,3,4);/q-1;;;+4/p-2/b39-27+,40-28+,41-27+,42-28+,45-31+,46-32+,49-31-,49-43-,50-32-,50-44-;;;

SMILES Code: CCC1=C2N3C(C=C4C(CCCO)=C(C)C(C=[N]5C6=C7C=C(OCCOCCOCCOC)C(OCCOCCOCCOC)=C6)=[N]4[Lu+3]358([O-]C(C)=O)([O-]C(C)=O)[N]9=C(C=[N]78)C(C)=C(CCCO)C9=C2)=C1CC

Appearance:
Black Solid powder

Purity:
>95 % (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:
Soluble in water

Shelf Life:
>2 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).

HS Tariff Code:
2934.99.9001

Preparing Stock Solutions

The following data is based on the product molecular weight 1166.12 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.

Select a batch to recalculate based on the batch molecular weight:
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

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1: Busch TM, Wang HW, Wileyto EP, Yu G, Bunte RM. Increasing damage to tumor blood vessels during motexafin lutetium-PDT through use of low fluence rate. Radiat Res. 2010 Sep;174(3):331-40. PubMed PMID: 20726728; PubMed Central PMCID: PMC2995951.

2: Patel H, Mick R, Finlay J, Zhu TC, Rickter E, Cengel KA, Malkowicz SB, Hahn SM, Busch TM. Motexafin lutetium-photodynamic therapy of prostate cancer: short- and long-term effects on prostate-specific antigen. Clin Cancer Res. 2008 Aug 1;14(15):4869-76. PubMed PMID: 18676760; PubMed Central PMCID: PMC2680073.

3: Wang HW, Finlay JC, Lee K, Zhu TC, Putt ME, Glatstein E, Koch CJ, Evans SM, Hahn SM, Busch TM, Yodh AG. Quantitative comparison of tissue oxygen and motexafin lutetium uptake by ex vivo and noninvasive in vivo techniques in patients with intraperitoneal carcinomatosis. J Biomed Opt. 2007 May-Jun;12(3):034023. PubMed PMID: 17614731.

4: Finlay JC, Zhu TC, Dimofte A, Stripp D, Malkowicz SB, Busch TM, Hahn SM. Interstitial fluorescence spectroscopy in the human prostate during motexafin lutetium-mediated photodynamic therapy. Photochem Photobiol. 2006 Sep-Oct;82(5):1270-8. PubMed PMID: 16808592.

5: Du KL, Mick R, Busch TM, Zhu TC, Finlay JC, Yu G, Yodh AG, Malkowicz SB, Smith D, Whittington R, Stripp D, Hahn SM. Preliminary results of interstitial motexafin lutetium-mediated PDT for prostate cancer. Lasers Surg Med. 2006 Jun;38(5):427-34. PubMed PMID: 16788929.

6: Ross HM, Smelstoys JA, Davis GJ, Kapatkin AS, Del Piero F, Reineke E, Wang H, Zhu TC, Busch TM, Yodh AG, Hahn SM. Photodynamic therapy with motexafin lutetium for rectal cancer: a preclinical model in the dog. J Surg Res. 2006 Oct;135(2):323-30. Epub 2006 May 2. PubMed PMID: 16650871.

7: Verigos K, Stripp DC, Mick R, Zhu TC, Whittington R, Smith D, Dimofte A, Finlay J, Busch TM, Tochner ZA, Malkowicz S, Glatstein E, Hahn SM. Updated results of a phase I trial of motexafin lutetium-mediated interstitial photodynamic therapy in patients with locally recurrent prostate cancer. J Environ Pathol Toxicol Oncol. 2006;25(1-2):373-87. PubMed PMID: 16566729.

8: Yeung PF. Motexafin lutetium (Pharmacyclics). IDrugs. 2001 Mar;4(3):351-9. PubMed PMID: 16025394.

9: Zhu TC, Finlay JC, Hahn SM. Determination of the distribution of light, optical properties, drug concentration, and tissue oxygenation in-vivo in human prostate during motexafin lutetium-mediated photodynamic therapy. J Photochem Photobiol B. 2005 Jun 1;79(3):231-41. Epub 2004 Dec 2. PubMed PMID: 15896650.

10: Miles D, Mody TD, Hatcher LI, Fiene J, Stiles M, Lin PP, Lee JW. Quantitation of motexafin lutetium in human plasma by liquid chromatography-tandem mass spectrometry and inductively coupled plasma-atomic emission spectroscopy. AAPS PharmSci. 2003;5(3):E23. PubMed PMID: 14621958; PubMed Central PMCID: PMC2750933.

11: Kereiakes DJ, Szyniszewski AM, Wahr D, Herrmann HC, Simon DI, Rogers C, Kramer P, Shear W, Yeung AC, Shunk KA, Chou TM, Popma J, Fitzgerald P, Carroll TE, Forer D, Adelman DC. Phase I drug and light dose-escalation trial of motexafin lutetium and far red light activation (phototherapy) in subjects with coronary artery disease undergoing percutaneous coronary intervention and stent deployment: procedural and long-term results. Circulation. 2003 Sep 16;108(11):1310-5. Epub 2003 Aug 25. PubMed PMID: 12939212.

12: Zhu TC, Hahn SM, Kapatkin AS, Dimofte A, Rodriguez CE, Vulcan TG, Glatstein E, Hsi RA. In vivo optical properties of normal canine prostate at 732 nm using motexafin lutetium-mediated photodynamic therapy. Photochem Photobiol. 2003 Jan;77(1):81-8. PubMed PMID: 12856887.

13: Dimofte A, Zhu TC, Hahn SM, Lustig RA. In vivo light dosimetry for motexafin lutetium-mediated PDT of recurrent breast cancer. Lasers Surg Med. 2002;31(5):305-12. PubMed PMID: 12430147.

14: Chou TM, Woodburn KW, Cheong WF, Lacy SA, Sudhir K, Adelman DC, Wahr D. Photodynamic therapy: applications in atherosclerotic vascular disease with motexafin lutetium. Catheter Cardiovasc Interv. 2002 Nov;57(3):387-94. Review. PubMed PMID: 12410519.

15: Solonenko M, Cheung R, Busch TM, Kachur A, Griffin GM, Vulcan T, Zhu TC, Wang HW, Hahn SM, Yodh AG. In vivo reflectance measurement of optical properties, blood oxygenation and motexafin lutetium uptake in canine large bowels, kidneys and prostates. Phys Med Biol. 2002 Mar 21;47(6):857-73. PubMed PMID: 11936174.

16: Yamaguchi A, Woodburn KW, Hayase M, Hoyt G, Robbins RC. Photodynamic therapy with motexafin lutetium (Lu-Tex) reduces experimental graft coronary artery disease. Transplantation. 2001 Jun 15;71(11):1526-32. PubMed PMID: 11435960.

17: Chen Z, Woodburn KW, Shi C, Adelman DC, Rogers C, Simon DI. Photodynamic therapy with motexafin lutetium induces redox-sensitive apoptosis of vascular cells. Arterioscler Thromb Vasc Biol. 2001 May;21(5):759-64. PubMed PMID: 11348871.

18: Hsi RA, Kapatkin A, Strandberg J, Zhu T, Vulcan T, Solonenko M, Rodriguez C, Chang J, Saunders M, Mason N, Hahn S. Photodynamic therapy in the canine prostate using motexafin lutetium. Clin Cancer Res. 2001 Mar;7(3):651-60. PubMed PMID: 11297261.

19: Griffin GM, Zhu T, Solonenko M, Del Piero F, Kapakin A, Busch TM, Yodh A, Polin G, Bauer T, Fraker D, Hahn SM. Preclinical evaluation of motexafin lutetium-mediated intraperitoneal photodynamic therapy in a canine model. Clin Cancer Res. 2001 Feb;7(2):374-81. PubMed PMID: 11234893.

20: Hayase M, Woodbum KW, Perlroth J, Miller RA, Baumgardner W, Yock PG, Yeung A. Photoangioplasty with local motexafin lutetium delivery reduces macrophages in a rabbit post-balloon injury model. Cardiovasc Res. 2001 Feb 1;49(2):449-55. PubMed PMID: 11164855.

21: Parise RA, Miles DR, Egorin MJ. Sensitive high-performance liquid chromatographic assay for motexafin gadolinium and motexafin lutetium in human plasma. J Chromatogr B Biomed Sci Appl. 2000 Dec 1;749(2):145-52. PubMed PMID: 11145051.

22: Yamaguchi A, Woodburn KW, Hayase M, Robbins RC. Reduction of vein graft disease using photodynamic therapy with motexafin lutetium in a rodent isograft model. Circulation. 2000 Nov 7;102(19 Suppl 3):III275-80. PubMed PMID: 11082401.

23: Rockson SG, Kramer P, Razavi M, Szuba A, Filardo S, Fitzgerald P, Cooke JP, Yousuf S, DeVault AR, Renschler MF, Adelman DC. Photoangioplasty for human peripheral atherosclerosis: results of a phase I trial of photodynamic therapy with motexafin lutetium (Antrin). Circulation. 2000 Nov 7;102(19):2322-4. PubMed PMID: 11067782.



Additional Information

Motexafin lutetium is a texaphyrin, marketed as Antrin by Pharmacyclics Inc.  It is a photosensitiser for use in photodynamic therapy to treat skin conditions and superficial cancers. It has also been tested for use in photoangioplasty (photodynamic treatment of diseased arteries). It is photoactivated by 732 nm light which allows greater depth of penetration.