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PF-5274857 is a novel Smo antagonist that specifically binds to Smo with a K(i) of 4.6 ± 1.1 nmol/L and completely blocks the transcriptional activity of the downstream gene Gli1 with an IC(50) of 2.7 ± 1.4 nmol/L in cells. The μ-opioid receptor is weakly inhibited by PF-5274857 with a dissociation constant of 36 μM subsequently determined in a functional assay. PF-5274857 was orally available and metabolically stable in vivo. PF-5274857 shows significant dose-dependent tumor growth inhibition (TGI) and induces tumor regression at high doses(>10 mg/kg). PF-5274857 is a potentially attractive clinical candidate for the treatment of tumor types including brain tumors and brain metastasis driven by an activated Hedgehog (Hh) signaling pathway. PF-5274857 is also able to cross the blood–brain barrier in rats within 4 hours post-dose.
| Molecular Weight | 436.96 |
| Formula | C20H25ClN4O3S |
| CAS Number | 1373615-35-0 |
| Solubility (25°C) | DMSO 80 mg/mL Water 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Hedgehog Products |
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| Cyclopamine
Cyclopamine is a naturally occuring steroidal alkaloid that causes cyclopia by blocking sonic hedgehog signaling. |
| LY2940680
LY2940680 is a potent Hedgehog inhibitor with potential anticancer activity. |
| LDE225
LDE225 (NVP-LDE225; Sonidegib) is a Hedgehog signaling pathway inhibitor (via smoothened antagonism) with IC50 of 1.3 nM (mouse) and 2.5 nM (human), respectively. |
| Jervine
Jervine is a naturally occuring steroidal alkaloid that causes cyclopia by blocking sonic hedgehog signaling. |
| Ciliobrevin A
Ciliobrevin A (HPI-4) is a hedgehog (Hh) pathway antagonist. It blocks Sonic hedgehog (Shh)-induced Hh pathway activation (IC50 = 7 μM) downstream of Smo. |
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