| Identification | Back Directory | [Name]
PF-05274857 HCl | [CAS]
1613439-62-5 | [Synonyms]
PF-05274857 HCl
PF 5274857 hydiochloride
PF-05274857 hydrochloride ≥95%
1-[4-(5'-Chloro-3,5-dimethyl[2,4'-bipyridin]-2'-yl-1-piperazinyl]-3-(methylsulfonyl)-1-propanone hydrochloride
1-[4-[5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl]piperazin-1-yl]-3-methylsulfonylpropan-1-one:hydrochloride | [Molecular Formula]
C20H26Cl2N4O3S | [MDL Number]
MFCD24387542 | [MOL File]
1613439-62-5.mol | [Molecular Weight]
473.41 |
| Hazard Information | Back Directory | [Uses]
PF-05274857 is a Smo receptor antagonist which blocks Gli1 transcription in cells stimulated with Shh (sonic hedgehog). | [in vivo]
PF-5274857 (1-30 mg/kg; p.o. once daily for 6 days) shows robust antitumor efficacy and correlation between PK and PD in medulloblastoma allograft mice models[1].
PF-5274857 (10 mg/kg; i.h.) in the plasma is able to cross the blood-brain barrier in rats within 4 hours postdose[1].
PF-5274857 (10-100 mg/kg; p.o. once daily for 4 days) is able to target Smo in the brain leading to the downregulation of Hh pathway activity in the brain tumor[1].
PF-5274857 (30 mg/kg; p.o. once daily for 34 days) increases the survival rates of primary Ptch+/? p53?/? medulloblastoma mice[1].
PF-5274857 (5-30 mg/kg; p.o.) exhibits the apparent volume of distribution of 5.6±0.5 L/kg and the half-life (T1/2) of 1.7±0.1 hours[1]. | Animal Model: | Severe combined immunodeficient (SCID)-beige mice (6-8 weeks old) are genetically engineered[1] | | Dosage: | 0, 1, 5, 10, 30 mg/kg | | Administration: | P.o. once daily for 6 days | | Result: | Showed robust antitumor activity with an in vivo IC50 of 8.9±2.6 nM. |
| Animal Model: | Severe combined immunodeficient (SCID)-beige mice (6-8 weeks old)[1] | | Dosage: | 0, 5, 10, 30 mg/kg (Pharmacokinetic Analysis) | | Administration: | A single p.o. | | Result: | The apparent volume of distribution of 5.6±0.5 L/kg; the half-life (T1/2) of 1.7±0.1 hours. |
| [storage]
Desiccate at RT |
|
| Company Name: |
Lynnchem
|
| Tel: |
86-(0)29-85992781 17792393971 |
| Website: |
http://www.lynnchem.com/ |
| Company Name: |
Novachemistry
|
| Tel: |
44-20819178-90 02081917890 |
| Website: |
https://www.novachemistry.com/ |
| Company Name: |
BOC Sciences
|
| Tel: |
|
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
|