KC7F2 is a cell permeable potent hypoxia inducible factor-1 (HIF-1) pathway inhibitor, with IC50 of 20 μM in LN229-HRE-AP cells, and with potential as a cancer therapy agent. KC7F2 inhibits the activation of HIF-target genes such as carbonic anhydrase IX, matrix metalloproteinase 2 (MMP2), enolase 1, and endothelin 1. KC7F2 suppresses the protein accumulation of HIF-1 in cancer cell lines by inhibition of its protein synthesis at the translation level. KC7F2 is preferentially cytotoxicity to cancer cells, an effect that is increased in hypoxia.
| Molecular Weight | 570.38 |
| Formula | C16H16Cl4N2O4S4 |
| CAS Number | 927822-86-4 |
| Solubility (25°C) | DMSO 30 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 HIF Products |
|---|
| 3-Aminobenzoic acid
3-Aminobenzoic acid is a hypoxia-inducible factor-1α (HIF-1α) inhibitor. |
| Steppogenin
Steppogenin is a potent inhibitor of HIF-1α and DLL4, with IC50 values of 0.56 and 8.46 μM, respectively. |
| HIV-IN-7
Axl-IN-16 is a Axl inhibitor. |
| HIF-2α-IN-9
HIF-2α-IN-9 is an inhibitor ofHIF-2α. |
| PHD-IN-2
PHD-IN-2 is a PHD antagonist (IC50: < 5 nM). |
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