Other grades of this product :
| Glasdegib Basic information |
| Product Name: | Glasdegib | | Synonyms: | EOS-60832;PF 04449913;1-((2R,4R)-2-(1H-benzo[d]iMidazol-2-yl)-1-Methylpiperidin-4-yl)-3-(4-cyanophenyl)urea;N-[(2R,4R)-2-(1H-Benzimidazol-2-yl)-1-methyl-4-piperidinyl]-N'-(4-cyanophenyl)urea;Glasdegib (PF-04449913);N-[(2R,4R)-2-(1H-Benzimidazol-2-yl)-1-methyl-4-piperidinyl]-N'-(4-cyanophenyl)urea PF 04449913;Glasdegib;CS-1041 | | CAS: | 1095173-27-5 | | MF: | C21H22N6O | | MW: | 374.44 | | EINECS: | | Product Categories: | Inhibitors | | Mol File: | 1095173-27-5.mol |
| Glasdegib Chemical Properties |
| Melting point | >214°C (dec.) | | Boiling point | 633.4±55.0 °C(Predicted) | | density | 1.33±0.1 g/cm3(Predicted) | | storage temp. | -20°C Freezer | | solubility | DMSO (Slightly), Methanol (Slightly) | | form | Solid | | pka | 11.93±0.10(Predicted) | | color | Off-White |
| Glasdegib Usage And Synthesis |
| Uses | Glasdegib acts as a potent, orally biovailablesmoothened (Smo) inhibitor used in the treatment of cancer. | | Biological Activity | pf-04449913 is an orally bioavailable inhibitor of smoothened with ic50 value of 5nm [1].in the hedgehog (hh) signaling pathway, the combination of hh ligands and their receptor patched leads to the activation of smoothened and subsequently activation of three transcription factors gli1, gli2 and gli3. it then leads to the proliferation of cells. as an antagonist of smoothened, pf-04449913 is developed for treatment of cancer [1].pf-04449913 is found not to inhibit cytochrome p450 and is negative in ames and micronucleus assays suggesting it as a safe drug. in the preclinical studies, pf-04449913 shows a half-life of 30 h and an oral bioavailability of 55% in humans. it also has low plasma clearance of 1.03 ml/min/kg and moderate volume of distribution (2.7 l/kg) [1]. | | Biochem/physiol Actions | PF-04449913 maleate salt is also known as 1-((2R,4R)-2-(1H-benzo[d]imidazol-2-yl)-1-methylpiperidin-4-yl)-3-(4-cyanophenyl)urea. It increases the differentiation of blood cells from hematopoietic precursors of the lymph gland medullary zone. This human Smo inhibitor protein is now under clinical trials to treat myeloid malignancies.
PF-04449913 (Glasdegib) is an orally bioavailable Hedgehog pathway inhibitor. PF-04449913 acts by binidng Smoothened (Smo) and blocking signal transduction. PF-04449913 has an IC50 of 5 nM in the Gli-Luciferase assay. In a Phase I clinical trial in patients with advanced solid tumors, PF-04449913 caused disease stabilization in 34% of patients. | | references | [1] munchhof mj, li q, shavnya a, borzillo gv, boyden tl, jones cs, lagreca sd, martinez-alsina l, patel n, pelletier k, reiter la, robbins md, tkalcevic gt. discovery of pf-04449913, a potent and orally bioavailable inhibitor of smoothened. acs med chem lett. 2011 dec 21;3(2):106-11. |
| Glasdegib Preparation Products And Raw materials |
|
日本语
한국어
Français
Deutsch
España
Türkiye