Free shipping on all orders over $ 500

Glasdegib

Cat. No. M9205
Glasdegib Structure
Synonym:

PF-04449913

Size Price Availability Quantity
10mM*1mL in DMSO USD 120  USD120 In stock
5mg USD 105  USD105 In stock
10mg USD 175  USD175 In stock
25mg USD 365  USD365 In stock
50mg USD 630  USD630 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Glasdegib (PF-04449913) inhibits sonic hedgehog (Shh) stimulated luciferase expression in mouse embryonic fibroblasts with an IC50 of 6.8 nM. In vitro microsomal assays, PF-04449913 have high clearance in rat and low clearance in dog and human, without inhibiting any of the major cytochrome P450 isoforms.

In vivo, CD34+ cord blood engrafted NSG mice are treated with Glasdegib (PF-04449913), the frequency of human CD45+ cells, progenitors and both myeloid and lymphoid cell fate commitment remained comparable to vehicle treated controls indicating that unlike LSC, normal human HSC cell fate decisions are Hh pathway independent.

Chemical Information
Molecular Weight 374.44
Formula C21H22N6O
CAS Number 1095173-27-5
Solubility (25°C) DMSO: ≥ 65 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Sadarangani A, et al. J Transl Med. GLI2 inhibition abrogates human leukemia stem cell dormancy.

[2] Munchhof MJ, et al. ACS Med Chem Lett. Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened.

Related Smo Products
Glasdegib Maleate

Glasdegib Maleate is an orally bioavailable Smoothened (Smo) inhibitor with an IC50 value of 4 nM for studies related to acute myeloid leukemia.

MRT-81 

MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer.

Fluticasone

Fluticasone is a corticosteroid and Smo agonist with an IC50 of 99 nM, which activates the Hedgehog signaling pathway and promotes the proliferation of primary neural stem or precursor cells, and can be used in respiratory related studies.

HhAntag 

HhAntag is a specific, potent and orally active small molecule SMO antagonist of the Hh pathway.

PF-5274857 hydrochloride 

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.

  Catalog
Abmole Inhibitor Catalog




Keywords: Glasdegib, PF-04449913 supplier, Smo, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.