PF 5274857 hydrochloride

Pricing Availability   Qty
Cat.No. 5262 - PF 5274857 hydrochloride | C20H25ClN4O3S.HCl | CAS No. 1613439-62-5
Description: High affinity and selective Smoothened (Smo) receptor antagonist
Chemical Name: 1-[4-(5'-Chloro-3,5-dimethyl[2,4'-bipyridin]-2'-yl-1-piperazinyl]-3-(methylsulfonyl)-1-propanone hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

High affinity and selective Smoothened (Smo) receptor antagonist (Ki = 4.6 nM). Exhibits >1000-fold selectivity for Smo over a panel of other receptors, ion channels and enzymes. Inhibits Shh-induced Hedgehog signaling in MEF cells. Induces tumor regression in a medulloblastoma allograft mouse model. Orally available and brain penetrant.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Compound Libraries

PF 5274857 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 473.42
Formula C20H25ClN4O3S.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1613439-62-5
PubChem ID 90489027
InChI Key GULNFUQAVPTTQV-UHFFFAOYSA-N
Smiles CC1=CN=C(C2=CC(N3CCN(C(CCS(C)(=O)=O)=O)CC3)=NC=C2Cl)C(C)=C1.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 47.34 100
DMSO 47.34 100

Preparing Stock Solutions

The following data is based on the product molecular weight 473.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.11 mL 10.56 mL 21.12 mL
5 mM 0.42 mL 2.11 mL 4.22 mL
10 mM 0.21 mL 1.06 mL 2.11 mL
50 mM 0.04 mL 0.21 mL 0.42 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

References

References are publications that support the biological activity of the product.

Rohner et al (2011) Effective targeting of Hedgehog signaling in a medulloblastoma model with PF-5274857, a potent and selective Smoothened antagonist that penetrates the blood-brain barrier. Mol.Cancer Ther. 11 57 PMID: 22084163


If you know of a relevant reference for PF 5274857 hydrochloride, please let us know.

View Related Products by Product Action

View all Smoothened Receptor Antagonists

Keywords: PF 5274857 hydrochloride, PF 5274857 hydrochloride supplier, PF5274857, hydrochloride, high, affinity, selective, smoothened, Smo, receptor, antagonist, hedgehog, signaling, antitumor, brain, penetrant, orally, available, active, Smoothened, Receptors, Hedgehog, Signaling, 5262, Tocris Bioscience

Citations for PF 5274857 hydrochloride

Citations are publications that use Tocris products.

Currently there are no citations for PF 5274857 hydrochloride. Do you know of a great paper that uses PF 5274857 hydrochloride from Tocris? Please let us know.

Reviews for PF 5274857 hydrochloride

There are currently no reviews for this product. Be the first to review PF 5274857 hydrochloride and earn rewards!

Have you used PF 5274857 hydrochloride?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥1250 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling