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CPI-613(Devimistat )

Catalog No.: 51905
Cas No.: 95809-78-2
Purity : 98% 
51905 - CPI-613(Devimistat ) | CAS 95809-78-2

Catalog number : 51905

CAS number : 95809-78-2

分子式 : C22H28O2S2 

分子量 : 388.59 

Iupac 化学名称 : 6,8-bis(benzylthio)octanoic acid, OCTANOIC ACID, 6,8-BIS((PHENYLMETHYL)THIO)-, (+/-)-6,8-BIS(BENZYLTHIO)OCTANOIC ACID

Smile : O=C(O)CCCCC(SCC1=CC=CC=C1)CCSCC2=CC=CC=C2

InChiKey : ZYRLHJIMTROTBO-UHFFFAOYSA-N

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同义词CPI-613;CPI613;CPI 613 ;Devimistat
英文同义词CPI-613;CPI613;CPI 613 ;Devimistat
分子式C22H28O2S2 
分子量388.59 
外观off-white solid 
纯度98% 
可溶性5mg/ml in DMSO 
存储3 years -20ºCpowder 
运输条件Shipped under ambient temperature. 
SmileO=C(O)CCCCC(SCC1=CC=CC=C1)CCSCC2=CC=CC=C2
InChiKeyZYRLHJIMTROTBO-UHFFFAOYSA-N
InChiInChI=1S/C22H28O2S2/c23-22(24)14-8-7-13-21(26-18-20-11-5-2-6-12-20)15-16-25-17-19-9-3-1-4-10-19/h1-6,9-12,21H,7-8,13-18H2,(H,23,24)
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1. CPI-613(Devimistat ) is an E1  pyruvate dehydrogenase (PDH) modulator that prevents cancer cells from metabolizing glucose for energy. CPI-613 has been granted orphan drug status by the US FDA for pancreatic cancer.

CPI-613(Devimistat ) is a first in class agent that targets mitochondrial metabolism through inhibition of pyruvate dehydrogenase and a-ketogluterate dehydrogenase.

 2. CPI-613(Devimistat ) is a lipoate derivative synthesized to be catalytically inert but to potentially mimic lipoate catalytic intermediates. The drug is in phase II of clinical trials for the treatment of Myelodysplastic syndromes; Pancreatic cancer; Small cell lung cancer; Solid tumors; Bile duct cancer; Acute Myeloid leukemia. The mechanism of CPI-613(Devimistat ) action can be explained by (I) inhibition of tumor cell pyruvate dehydrogenase complex (PDC) through activation of pyruvate dehydrogenase kinases leading to inactivating phosphorylation of the E1alpha-subunit of PDC; and (II) inhibition of alpha-ketoglutarate dehydrogenase.

3. Application.

In Vivo Use Guide 
Patients with bile duct cancer receive CPI-613(Devimistat ) IV over 2 hours on days 1-5, 1 week prior to course. After that, they receive the drug IV over 2 hours on days 1 and 4 of weeks 1-3. Treatment repeats every 4 weeks for up to 2 courses. Patients with pancreatic cancer, small cell lung cancer, AML, and Myelodysplastic Syndrome receive 3,000 mg/m2 CPI-613 infused IV over 2 hours on Days 1 and 4 of each of the 3 treatment weeks.
Route of Administration: Intravenous
In Vitro Use Guide 
In the ATP production assay, H460 cells were seeded at 10,000 cells per well in RPMI (11 mM glucose, 2 mM glutamine) medium and grown overnight. The medium was then changed to RPMI without glucose and containing 10 mM pyruvate and 2 mM glutamine alone or together with 0.1 mM water soluble oleic acid. After 24 hours, the medium was replaced with fresh RPMI without glucose and containing either 10 mM pyruvate and 2 mM glutamine or 0.1 mM oleic acid and 0.5 mM aspartate (matched to overnight adaptation) and containing CPI-613(Devimistat ) (240 uM) in the treated samples for 2 hours before ATP level measurements.


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