CBR 5884 is a 3-Phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50 = 33 μM). Decreases de novo serine synthesis in cancer cells. Inhibits proliferation of cancer cell lines having high PHGDH expression levels.
| Molecular Weight | 336.39 |
| Formula | C14H12N2O4S2 |
| CAS Number | 681159-27-3 |
| Solubility (25°C) | DMSO 33.64 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related PHGDH Products |
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| PKUMDL-WQ-2101
PKUMDL-WQ-2101 is a non-NAD+-competing allosteric phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 34.8 μM. PKUMDL-WQ-2101 exhibits antitumor activity. |
| PHGDH-inactive
PHGDH-inactive has no activity against PHGDH and serves as a negative control of NCT-502 and NCT-503. |
| NCT-502
NCT-502 is a human phosphoglycerate dehydrogenase (PHGDH) inhibitor, cytotoxic to PHGDH-dependent cancer cells, and reduces glucose-derived serine production, with an IC50 of 3.7 μM against PHGDH. |
| BI-4924
BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. |
| BI-4916
BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD+-competitive PHGDH inhibitor. |
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