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

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

MedKoo CAT#: 208289

CAS#: 1131626-47-5

Description: 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

Instruction

Theoretical Analysis

MedKoo Cat#: 208289
Name: Gamitrinib hexafluorophosphate
CAS#: 1131626-47-5
Chemical Formula: C52H65F6N3O8P2
Exact Mass: 1,035.42
Molecular Weight: 1,036.040
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 1250	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Gamitrinib-hexafluorophosphate, Gamitrinibhexafluorophosphate, Gamitrinib 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

Biological target:
In vitro activity:
In vivo activity:

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

Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.

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