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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
CPI-613 is a novel anti-tumor compound targeting on PDH. CPI-613 at concentration of 240μM disrupted H460 cancer cell mitochondrial metabolism including inhibition of PDH complex activity, and caused loss of mitochondrial membrane potential. It induced extensive post-translational modification of PDH E1 at 300μM, which is acquired high PDK levels. CPI-613 demonstrated anticancer activity both in vitro and in vivo. It induced both apoptotic and non-apoptotic cell death in H460 human lung cancer and Saos-2 human sarcoma cells at concentration of 240μM in 22 or 24h. It showed strong antitumor activity against human non-small cell lung and pancreatic cancers in xenograft models at dose of 25mg/kg[4]. CPI-613 undergoes both phase 1 (oxidation) and phase 2 (glucuronidation) transformations[5]. Inhibition of KGDH by CPI-613 may partially contribute to antitumor activity of CPI-613. It inhibited KGDH function strongly and rapidly, selectively in tumor cells. Moreover, CPI-613 induced a correspondingly rapid, powerful redox signal in tumor cell mitochondria[6].
Devimistat 细胞实验
Cell Line
Concentration
Treated Time
Description
References
HN6
100 µM
24 hours
To evaluate the effect of CPI-613 on ATP production in HNSCC cells, results showed that CPI-613 reduced ATP production
J Exp Clin Cancer Res. 2021 Dec 14;40(1):393.
HN31
100 µM
24 hours
To evaluate the effect of CPI-613 on ATP production in HNSCC cells, results showed that CPI-613 reduced ATP production
J Exp Clin Cancer Res. 2021 Dec 14;40(1):393.
KNS42 cells
100 µM
24 hours
To evaluate the effect of CPI-613 on the transcriptome of KNS42 cells, the results showed that CPI-613 suppressed gene sets related to oxidative phosphorylation and respiratory chain complexes.
JCI Insight. 2024 Mar 14;9(8):e172565.
Sk-Mel-5
300 µM
24 hours
To detect the effect of CPI613 on glycolysis levels, the results showed that CPI613 significantly increased glycolysis levels, glycolytic capacity, and glycolytic reserve.
J Immunother Cancer. 2023 Sep;11(9):e007146.
Pa03C
50 µM
24 hours
To evaluate the effect of Devimistat on pancreatic cancer cell metabolism, results showed that Devimistat significantly reduced the utilization of TCA cycle substrates.
J Exp Clin Cancer Res. 2021 Aug 10;40(1):251.
Panc10.05
50 µM
24 hours
To evaluate the effect of Devimistat on pancreatic cancer cell metabolism, results showed that Devimistat significantly reduced the utilization of TCA cycle substrates.
J Exp Clin Cancer Res. 2021 Aug 10;40(1):251.
B16F10
300 µM
48 hours
To detect the effect of CPI613 on PD-L1 mRNA expression, the results showed that CPI613 significantly upregulated PD-L1 mRNA expression.
J Immunother Cancer. 2023 Sep;11(9):e007146.
MCF7
150 µM
48 hours
To evaluate the effect of CPI-613 on breast cancer cells, the results showed that the combination of CPI-613 with FRI-1 significantly increased cell death.
Antioxidants (Basel). 2021 Oct 14;10(10):1618.
MDA-MB-231
150 µM
48 hours
To evaluate the effect of CPI-613 on breast cancer cells, the results showed that the combination of CPI-613 with FRI-1 significantly increased cell death.
Antioxidants (Basel). 2021 Oct 14;10(10):1618.
UWB1.289 MUT
75 µM
7 days
CPI-613 treatment decreased CD133+ and CD117+ cell frequency and reduced sphere-forming capacity.
Cancers (Basel). 2019 Oct 29;11(11):1678.
OVCAR3
75 µM
7 days
CPI-613 treatment decreased CD133+ and CD117+ cell frequency and reduced sphere-forming capacity.
Cancers (Basel). 2019 Oct 29;11(11):1678.
PANC-1 cells
1, 10, 50 µM
72 hours
To evaluate the cytotoxicity of CPI-613 on PANC-1 cells, results showed that CPI-613 exhibited cytotoxicity at different concentrations.
ACS Appl Mater Interfaces. 2019 Dec 11;11(49):45390-45403.
PaTu-8902 cells
50 µM
72 hours
CPI-613 selectively kills cells adapted to acidosis through inhibition of the Krebs cycle and induction of oxidative stress, even in the presence of lactate.
Int J Mol Sci. 2021 Oct 6;22(19):10790.
HeLa cells
50 µM
72 hours
CPI-613 selectively kills cells adapted to acidosis through inhibition of the Krebs cycle and induction of oxidative stress, even in the presence of lactate.
Int J Mol Sci. 2021 Oct 6;22(19):10790.
Hep G2 cells
50 µM
72 hours
CPI-613 selectively kills cells adapted to acidosis through inhibition of the Krebs cycle and induction of oxidative stress, even in the presence of lactate.
Int J Mol Sci. 2021 Oct 6;22(19):10790.
HDF cells
50 µM
72 hours
CPI-613 selectively kills cells adapted to acidosis through inhibition of the Krebs cycle and induction of oxidative stress, even in the presence of lactate.
Int J Mol Sci. 2021 Oct 6;22(19):10790.
Devimistat 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
NOD/SCID mice
OVCAR3 xenograft model
Intraperitoneal injection
12.5 mg/kg
Once weekly for 2 weeks
CPI-613 treatment decreased CD133+ and CD117+ cell frequency and inhibited tumor growth.
Cancers (Basel). 2019 Oct 29;11(11):1678.
NSG mice
Tongue tumor model
Intraperitoneal injection
25 mg/kg
Every 3 days for 2 weeks
To evaluate the therapeutic effect of CPI-613 on the tongue tumor model, results showed that CPI-613 significantly inhibited tumor growth
J Exp Clin Cancer Res. 2021 Dec 14;40(1):393.
Nude mice
GBM12 xenograft model
Intraperitoneal injection
50 mg/kg
3 times per week, continuous treatment
To evaluate the tumor growth inhibitory effect of CPI-613 combined with ABT263 in the GBM12 xenograft model, the results showed that the combination treatment significantly inhibited tumor growth.
JCI Insight. 2024 Mar 14;9(8):e172565.
NOD/SCIDγ(-/-) mice
Pancreatic cancer xenograft model
Oral
50 mg/kg
Twice daily for 15 or 20 days
To evaluate the antitumor effect of Devimistat on pancreatic cancer xenograft models, results showed that Devimistat significantly reduced tumor volume and weight.
J Exp Clin Cancer Res. 2021 Aug 10;40(1):251.
Mice
Orthotopic pancreatic cancer model
Intravenous injection
CPI-613 10 mg/kg, LY2109761 13.2 mg/kg
Every 5 days for a total of 6 injections
To evaluate the antitumor efficacy of the nanopolyplexes in a pancreatic cancer mouse model, results showed that the p-PPCL nanopolyplex significantly inhibited tumor growth.
ACS Appl Mater Interfaces. 2019 Dec 11;11(49):45390-45403.
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