Gamitrinib hexafluorophosphate | CAS#1131626-47-5 | Inhibitor

MedKoo Cat#: 208289 | Name: Gamitrinib hexafluorophosphate

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Description:

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

Gamitrinib hexafluorophosphate is a mitochondrial-localized HSP90 inhibitor. Preclinical findings established the therapeutic role of Gamitrinib in gliomas and revealed the inhibition of mitochondrial biogenesis and tumor bioenergetics as the primary antitumor mechanisms in gliomas.

Chemical Structure

Gamitrinib hexafluorophosphate

CAS#1131626-47-5

Theoretical Analysis

MedKoo Cat#: 208289

Name: Gamitrinib hexafluorophosphate

CAS#: 1131626-47-5

Chemical Formula: C52H65F6N3O8P2

Exact Mass: 0.0000

Molecular Weight: 1036.04

Elemental Analysis: C, 60.28; H, 6.32; F, 11.00; N, 4.06; O, 12.35; P, 5.98

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 1,250.00	2 Weeks

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Related CAS #

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Synonym

Gamitrinib-hexafluorophosphate, Gamitrinibhexafluorophosphate, Gamitrinib Hexafluorophosphate; G-TPP Hexafluorophosphate; Gamitrinib TPP hexafluorophosphate

IUPAC/Chemical Name

(6-(((4E,6Z,8S,9S,10E,12S,13R,14S,16R)-9-(Carbamoyloxy)-13-hydroxy-8,14-dimethoxy-4,10,12,16-tetramethyl-3,20,22-trioxo-2-azabicyclo[16.3.1]docosa-1(21),4,6,10,18-pentaen-19-yl)amino)hexyl)triphenylphosphonium hexafluorophosphate

InChi Key

NFIBTCZSRLMDOD-WLXHSWTPSA-O

InChi Code

InChI=1S/C52H64N3O8P.F6P/c1-35-31-42-47(54-29-18-7-8-19-30-64(39-22-12-9-13-23-39,40-24-14-10-15-25-40)41-26-16-11-17-27-41)44(56)34-43(49(42)58)55-51(59)36(2)21-20-28-45(61-5)50(63-52(53)60)38(4)33-37(3)48(57)46(32-35)62-6;1-7(2,3,4,5)6/h9-17,20-28,33-35,37,45-46,48,50,57H,7-8,18-19,29-32H2,1-6H3,(H3-,53,54,55,56,58,59,60);/q;-1/p+1/b28-20-,36-21+,38-33+;/t35-,37+,45+,46+,48-,50+;/m1./s1

SMILES Code

O=C1C(NC(/C(C)=C/C=C\[C@H](OC)[C@@H](OC(N)=O)/C(C)=C/[C@H](C)[C@@H](O)[C@@H](OC)C[C@H](C)CC1=C2NCCCCCC[P+](C3=CC=CC=C3)(C4=CC=CC=C4)C5=CC=CC=C5)=O)=CC2=O.F[P-](F)(F)(F)(F)F

Appearance

Solid powder

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 1,036.04 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

1: Wei S, Yin D, Yu S, Lin X, Savani MR, Du K, Ku Y, Wu D, Li S, Liu H, Tian M, Chen Y, Bowie M, Hariharan S, Waitkus M, Keir ST, Sugarman ET, Deek RA, Labrie M, Khasraw M, Lu Y, Mills GB, Herlyn M, Wu K, Liu L, Wei Z, Flaherty KT, Abdullah K, Zhang G, Ashley DM. Antitumor Activity of a Mitochondrial-Targeted HSP90 Inhibitor in Gliomas. Clin Cancer Res. 2022 May 13;28(10):2180-2195. doi: 10.1158/1078-0432.CCR-21-0833. PMID: 35247901. 2: Hayat U, Elliott GT, Olszanski AJ, Altieri DC. Feasibility and safety of targeting mitochondria for cancer therapy - preclinical characterization of gamitrinib, a first-in-class, mitochondriaL-targeted small molecule Hsp90 inhibitor. Cancer Biol Ther. 2022 Dec 31;23(1):117-126. doi: 10.1080/15384047.2022.2029132. PMID: 35129069; PMCID: PMC8820820. 3: Wang N, Zhu P, Huang R, Sun L, Dong D, Gao Y. Suppressing TRAP1 sensitizes glioblastoma multiforme cells to temozolomide. Exp Ther Med. 2021 Nov;22(5):1246. doi: 10.3892/etm.2021.10681. Epub 2021 Sep 2. PMID: 34539842; PMCID: PMC8438667. 4: Needham RJ, Bridgewater HE, Romero-Canelón I, Habtemariam A, Clarkson GJ, Sadler PJ. Structure-activity relationships for osmium(II) arene phenylazopyridine anticancer complexes functionalised with alkoxy and glycolic substituents. J Inorg Biochem. 2020 Sep;210:111154. doi: 10.1016/j.jinorgbio.2020.111154. Epub 2020 Jun 24. PMID: 32771772. 5: Nguyen TTT, Zhang Y, Shang E, Shu C, Quinzii CM, Westhoff MA, Karpel-Massler G, Siegelin MD. Inhibition of HDAC1/2 Along with TRAP1 Causes Synthetic Lethality in Glioblastoma Model Systems. Cells. 2020 Jul 10;9(7):1661. doi: 10.3390/cells9071661. PMID: 32664214; PMCID: PMC7407106. 6: Zhang Y, Nguyen TTT, Shang E, Mela A, Humala N, Mahajan A, Zhao J, Shu C, Torrini C, Sanchez-Quintero MJ, Kleiner G, Bianchetti E, Westhoff MA, Quinzii CM, Karpel-Massler G, Bruce JN, Canoll P, Siegelin MD. MET Inhibition Elicits PGC1α-Dependent Metabolic Reprogramming in Glioblastoma. Cancer Res. 2020 Jan 1;80(1):30-43. doi: 10.1158/0008-5472.CAN-19-1389. Epub 2019 Nov 6. PMID: 31694905; PMCID: PMC6942623. 7: Nguyen TTT, Ishida CT, Shang E, Shu C, Bianchetti E, Karpel-Massler G, Siegelin MD. Activation of LXR Receptors and Inhibition of TRAP1 Causes Synthetic Lethality in Solid Tumors. Cancers (Basel). 2019 Jun 7;11(6):788. doi: 10.3390/cancers11060788. PMID: 31181660; PMCID: PMC6627953. 8: Agarwal E, Altman BJ, Seo JH, Ghosh JC, Kossenkov AV, Tang HY, Krishn SR, Languino LR, Gabrilovich DI, Speicher DW, Dang CV, Altieri DC. Myc-mediated transcriptional regulation of the mitochondrial chaperone TRAP1 controls primary and metastatic tumor growth. J Biol Chem. 2019 Jul 5;294(27):10407-10414. doi: 10.1074/jbc.AC119.008656. Epub 2019 May 16. PMID: 31097545; PMCID: PMC6615691. 9: Zhang C, Wang R, Liu Z, Bunker E, Lee S, Giuntini M, Chapnick D, Liu X. The plant triterpenoid celastrol blocks PINK1-dependent mitophagy by disrupting PINK1's association with the mitochondrial protein TOM20. J Biol Chem. 2019 May 3;294(18):7472-7487. doi: 10.1074/jbc.RA118.006506. Epub 2019 Mar 18. PMID: 30885942; PMCID: PMC6509500. 10: Reyes-Uribe P, Adrianzen-Ruesta MP, Deng Z, Echevarria-Vargas I, Mender I, Saheb S, Liu Q, Altieri DC, Murphy ME, Shay JW, Lieberman PM, Villanueva J. Exploiting TERT dependency as a therapeutic strategy for NRAS-mutant melanoma. Oncogene. 2018 Jul;37(30):4058-4072. doi: 10.1038/s41388-018-0247-7. Epub 2018 Apr 26. PMID: 29695835; PMCID: PMC6062502.