Product Name :
PF-5274857 hydrochloride
Description:
PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.
CAS:
1613439-62-5
Molecular Weight:
473.42
Formula:
C20H26Cl2N4O3S
Chemical Name:
1-(4-5′-chloro-3,5-dimethyl-[2,4′-bipyridin]-2′-ylpiperazin-1-yl)-3-methanesulfonylpropan-1-one hydrochloride
Smiles :
Cl.CS(=O)(=O)CCC(=O)N1CCN(CC1)C1C=C(C(Cl)=CN=1)C1=NC=C(C)C=C1C
InChiKey:
GULNFUQAVPTTQV-UHFFFAOYSA-N
InChi :
InChI=1S/C20H25ClN4O3S.ClH/c1-14-10-15(2)20(23-12-14)16-11-18(22-13-17(16)21)24-5-7-25(8-6-24)19(26)4-9-29(3,27)28;/h10-13H,4-9H2,1-3H3;1H
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
PF-5274857 hydrochloride is a potent, selective, orally active and brain-penetrant antagonist of Smo, with an IC50 of 5.8 nM and Ki of 4.6 nM. PF-5274857 hydrochloride has potential for research of tumor types including brain tumors and brain metastasis driven by an activated Hh pathway.|Product information|CAS Number: 1613439-62-5|Molecular Weight: 473.42|Formula: C20H26Cl2N4O3S|Chemical Name: 1-(4-5′-chloro-3,5-dimethyl-[2,4′-bipyridin]-2′-ylpiperazin-1-yl)-3-methanesulfonylpropan-1-one hydrochloride|Smiles: Cl.CS(=O)(=O)CCC(=O)N1CCN(CC1)C1C=C(C(Cl)=CN=1)C1=NC=C(C)C=C1C|InChiKey: GULNFUQAVPTTQV-UHFFFAOYSA-N|InChi: InChI=1S/C20H25ClN4O3S.ClH/c1-14-10-15(2)20(23-12-14)16-11-18(22-13-17(16)21)24-5-7-25(8-6-24)19(26)4-9-29(3,27)28;/h10-13H,4-9H2,1-3H3;1H|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.Travoprost medchemexpress |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|How to use|In Vitro:|PF-5274857 completely inhibits Shh-induced Hh pathway activity with an IC50 of 2.Esaxerenone Mineralocorticoid Receptor 7±1.PMID:33188646 4 nM measured by the transcriptional activity of Smo downstream gene Gli1 in MEF cells. PF-5274857 shows less than 20% inhibition against a broad panel of protein kinases at 1 μM.|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. PF-5274857 (10 mg/kg; i.h.) in the plasma is able to cross the blood-brain barrier in rats within 4 hours postdose. 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. PF-5274857 (30 mg/kg; p.o. once daily for 34 days) increases the survival rates of primary Ptch+/− p53−/− medulloblastoma mice. 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.|Products are for research use only. Not for human use.|
