store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Glutaminase-IN-1 (CB839 derivative), a novel 1,3,4-selenodiazepine renal-type glutaminase (KGA) variant inhibitor, showed antitumor activity in an aggressive H22 hepatocellular carcinoma xenograft model.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 49.00 | |
2 mg | In stock | $ 68.00 | |
5 mg | In stock | Inquiry | |
25 mg | In stock | Inquiry |
Description | Glutaminase-IN-1 (CB839 derivative), a novel 1,3,4-selenodiazepine renal-type glutaminase (KGA) variant inhibitor, showed antitumor activity in an aggressive H22 hepatocellular carcinoma xenograft model. |
Targets&IC50 | A549 cells:17 nM, KGA:1 nM, HCT116 cells:9 nM, Caki-1 cells:19 nM, H2:6.78 μM |
In vitro | Glutaminase-IN-1 (CPD20) is a derivative of CB839, serving as a conformational inhibitor of kidney-type glutaminase (KGA) with an IC50 of 1 nM. Glutaminase-IN-1 exhibits improved cellular uptake and anti-tumor activity. The IC50 values of Glutaminase-IN-1 in A549, H2, Caki-1, and HCT116 cell lines are 17 nM, 6.78 μM, 19 nM, and 9 nM, respectively. Glutaminase-IN-1 demonstrates superior KGA inhibitory activity compared to the corresponding BPTES and CB839[1]. |
In vivo | Glutaminase-IN-1 (10 mg/kg, subcutaneous) reduced the size and weight of HCT116 tumors, and statistical analysis indicated a significant 40% reduction in tumor weight with CPD20. Glutaminase-IN-1 significantly prolonged the survival of mice carrying H22[1]. |
Synonyms | CB839 derivative |
Molecular Weight | 618.47 |
Formula | C26H24F3N7O3Se |
CAS No. | 2247127-79-1 |
store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 100 mg/mL (161.69 mM), Sonication is recommended.
H2O: 1 mg/mL (1.61 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. More
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Glutaminase-IN-1 2247127-79-1 Metabolism transporter GlutaminaseIN1 CB839 derivative Glutaminase IN 1 inhibitor inhibit