HLM006474 is a pan E2F inhibitor, which inhibits E2F4 DNA-binding with an IC50 of 29.8 µM in A375 cells. HLM006474 reduces E2F4 protein levels in A375 melanoma cells. HLM006474 induces apoptosis of A375 and MDA-MB-231 breast cancer cells. HLM006474 inhibits A375 proliferation and invasion in a three dimensional skin model of A375 invasion. HLM006474 also attenuates human embryonic stem cell proliferation.
HLM006474 reduces the viability of both SCLC and NSCLC lines with a biological IC50 that varies between 15 and 75 mM, but with no significant difference between the groups. HLM006474 leads to a decrease in the mRNA levels of MAD2. Furthmore, HLM006474 apparently suppresses the increase of Mad2 protein and pRb-S780 signal but not the level of Skp2 protein in human lung cancer A549 cells.
In vivo, HLM006474 leads to significant downregulation of E2F4 protein. Short exposure of Chx10Cre;Rbf/f;p107−/− embryos to HLM006474 has a dramatic effect on tumorigenesis.
| Molecular Weight | 399.48 |
| Formula | C25H25N3O2 |
| CAS Number | 353519-63-8 |
| Solubility (25°C) | DMSO 10 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.
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