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MedKoo Cat#: 201942 | Name: Motexafin lutetium hydrate
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Description:

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

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

Motexafin lutetium hydrate
Motexafin lutetium hydrate
CAS#156436-90-7 (lutetium hydrate)

Theoretical Analysis

MedKoo Cat#: 201942

Name: Motexafin lutetium hydrate

CAS#: 156436-90-7 (lutetium hydrate)

Chemical Formula: C52H74LuN5O15

Exact Mass: 0.0000

Molecular Weight: 1166.12

Elemental Analysis: C, 53.56; H, 6.22; Lu, 15.00; N, 6.01; O, 19.21

Price and Availability

Size Price Availability Quantity
1mg USD 250.00 Ready to ship
2mg USD 450.00 Ready to ship
5mg USD 950.00 Ready to ship
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Related CAS #
156436-90-7 (lutetium hydrate) 246252-06-2 (gadolinium) 189752-49-6 (free)
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
More Info
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.         
Biological target:
Motexafin lutetium is a pentadentate aromatic metallotexaphyrin with photosensitizing properties.
In vitro activity:
In vivo activity:
The purpose was to determine the feasibility of comprehensive treatment of the canine prostate with photodynamic therapy (PDT) using motexafin lutetium (Lu-Tex) and to evaluate the toxicity and tissue effects associated with this treatment. Twenty-five adult male beagles with normal prostate glands were given an i.v. injection of the second-generation photosensitizer Lu-Tex (2–6 mg/kg). An apparent allergic reaction to the photosensitizer injection was noted in 10 of 14 dogs receiving 6 mg/kg Lu-Tex. Based on these initial results, the light fluence was escalated to 150 J/cm at a fluence rate of 150 mW/cm and the Lu-Tex dose remained at 6 mg/kg. The next experiments were designed to evaluate the acute (2 days after PDT) clinical and histological effects from this increased light fluence. Based on these results, the doses of Lu-Tex and light were decreased. A total of 11 dogs were treated with Lu-Tex 2 mg/kg, with a light fluence of 100 J/cm at a fluence rate of 150 mW/cm. No acute or long-term clinical toxicities were observed. The results of this study demonstrated that Lu-Tex PDT is feasible in the canine prostate. Reference: Clin Cancer Res. 2001 Mar;7(3):651-60. https://pubmed.ncbi.nlm.nih.gov/11297261/
Solvent mg/mL mM
Solubility
Soluble in water 0.0 0.00
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 1,166.12 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.

Recalculate based on batch purity %
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:
1. 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. PMID: 11297261. 2. 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. PMID: 11234893.
In vitro protocol:
TBD
In vivo protocol:
1. 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. PMID: 11297261. 2. 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. PMID: 11234893.
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PMID: 26667346. 12: Qiu L, Zhang F, Shi Y, Bai Z, Wang J, Li Y, Lee D, Ingraham C, Feng X, Yang X. Gliomas: Motexafin Gadolinium-enhanced Molecular MR Imaging and Optical Imaging for Potential Intraoperative Delineation of Tumor Margins. Radiology. 2016 May;279(2):400-9. doi: 10.1148/radiol.2015150895. Epub 2015 Nov 24. PMID: 26599802; PMCID: PMC4851136. 13: Finlay JC, Zhu TC, Dimofte A, Stripp D, Malkowicz SB, Whittington R, Miles J, Glatstein E, Hahn SM. In vivo determination of the absorption and scattering spectra of the human prostate during photodynamic therapy. Proc SPIE Int Soc Opt Eng. 2014 Jun 14;5315:132-142. doi: 10.1117/12.528968. PMID: 26146442; PMCID: PMC4489148. 14: Zhang F, Bai Z, Shi Y, Wang J, Li Y, Yang X. Interventional MRI-guided local delivery of agents into swine bile duct walls using MR-compatible needle- integrated balloon catheter system. NMR Biomed. 2015 Jun;28(6):679-84. doi: 10.1002/nbm.3308. Epub 2015 Apr 22. 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Large-scale Dirac-Fock-Breit method using density fitting and 2-spinor basis functions. J Chem Phys. 2013 May 28;138(20):204113. doi: 10.1063/1.4807612. PMID: 23742460. 19: Meng Y, Wang J, Sun J, Zhang F, Willis P, Li J, Wang H, Zhang T, Soriano S, Qiu B, Yang X. 3.0-T MR imaging of intracoronary local delivery of motexafin gadolinium into coronary artery walls. Radiology. 2013 Aug;268(2):556-62. doi: 10.1148/radiol.13121451. Epub 2013 Mar 19. PMID: 23513243; PMCID: PMC3721057. 20: Wang H, Zhang F, Meng Y, Zhang T, Willis P, Le T, Soriano S, Ray E, Valji K, Zhang G, Yang X. MRI-monitored intra-shunt local agent delivery of motexafin gadolinium: towards improving long-term patency of TIPS. PLoS One. 2013;8(2):e57419. doi: 10.1371/journal.pone.0057419. Epub 2013 Feb 28. PMID: 23468986; PMCID: PMC3585394.