PF-05274857 HCl
- Product Name
- PF-05274857 HCl
- CAS No.
- 1613439-62-5
- Chemical Name
- PF-05274857 HCl
- 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-3,5-dimethyl-[2,4'-bipyridin]-2'-yl)piperazin-1-yl)-3-(methylsulfonyl)propan-1-one hydrochloride;1-[4-[5-chloro-4-(3,5-dimethylpyridin-2-yl)pyridin-2-yl]piperazin-1-yl]-3-methylsulfonylpropan-1-one:hydrochloride
- CBNumber
- CB63067569
- Molecular Formula
- C20H26Cl2N4O3S
- Formula Weight
- 473.41
- MOL File
- 1613439-62-5.mol
PF-05274857 HCl Property
- storage temp.
- Store at -20°C
- solubility
- DMSO (Slightly, Heated), Water (Slightly)
- form
- Solid
- color
- Light Yellow
N-Bromosuccinimide Price
- Product number
- 15022
- Product name
- PF-05274857 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 1mg
- Price
- $25
- Updated
- 2021/12/16
- Product number
- 15022
- Product name
- PF-05274857 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 5mg
- Price
- $81
- Updated
- 2021/12/16
- Product number
- 15022
- Product name
- PF-05274857 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 10mg
- Price
- $150
- Updated
- 2021/12/16
- Product number
- 15022
- Product name
- PF-05274857 (hydrochloride)
- Purity
- ≥98%
- Packaging
- 25mg
- Price
- $313
- Updated
- 2021/12/16
- Product number
- P227585
- Product name
- PF-05274857Hydrochloride
- Packaging
- 10mg
- Price
- $385
- Updated
- 2021/12/16
PF-05274857 HCl Chemical Properties,Usage,Production
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
PF-05274857 HCl Preparation Products And Raw materials
Raw materials
Preparation Products
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