Glasdegib
- CAS No.
- 1095173-27-5
- Chemical Name:
- Glasdegib
- Synonyms
- CS-1041;EOS-60832;Glasdegib;PF 04449913;Glasdegib-D3;Glasdegib-D4;Glasdegib-13C6;Glasdegib-13C,15N;Glasdegib USP/EP/BP;PF04449913; PF 04449913
- CBNumber:
- CB82658197
- Molecular Formula:
- C21H22N6O
- Molecular Weight:
- 374.44
- MDL Number:
- MFCD25976839
- MOL File:
- 1095173-27-5.mol
| 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) |
| pka | 11.93±0.10(Predicted) |
| form | Solid |
| color | Off-White |
| InChIKey | SFNSLLSYNZWZQG-VQIMIIECSA-N |
| SMILES | N([C@@H]1CCN(C)[C@@H](C2NC3=CC=CC=C3N=2)C1)C(NC1=CC=C(C#N)C=C1)=O |
| FDA UNII | K673DMO5H9 |
| ATC code | L01XJ03 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS08 |
|---|---|
| Signal word | Warning |
| Hazard statements | H361-H373 |
| Precautionary statements | P201-P202-P281-P308+P313-P405-P501-P260-P314-P501 |
Glasdegib price More Price(23)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Cayman Chemical | 9002936 | PF-04449913 ≥98% | 1095173-27-5 | 1mg | $34 | 2024-03-01 | Buy |
| Cayman Chemical | 9002936 | PF-04449913 ≥98% | 1095173-27-5 | 5mg | $109 | 2024-03-01 | Buy |
| Cayman Chemical | 9002936 | PF-04449913 ≥98% | 1095173-27-5 | 10mg | $198 | 2024-03-01 | Buy |
| Cayman Chemical | 9002936 | PF-04449913 | 1095173-27-5 | 25mg | $412 | 2024-03-01 | Buy |
| TRC | G406550 | Glasdegib | 1095173-27-5 | 5mg | $135 | 2021-12-16 | Buy |
Glasdegib Chemical Properties,Uses,Production
Uses
Glasdegib acts as a potent, orally biovailablesmoothened (Smo) inhibitor used in the treatment of cancer.
Definition
ChEBI: Glasdegib is a member of the class of benzimidazoles that is 1H-benzimidazole which is substituted by a (2R,4S)-4-{[(4-cyanophenyl)carbamoyl]amino}-1-methylpiperidin-2-yl group at position 2. It is a hedgehog signalling pathway inhibitor that acts by binding to Smoothened (SMO) receptors and blocking signal transduction (IC50 = 5 nM). It is used in combination with low-dose cytarabine, for the treatment of newly-diagnosed acute myeloid leukemia (AML) in adult patients (aged >= 75 years), or who have medical conditions that prevent the use of standard chemotherapy. It has a role as a SMO receptor antagonist, a Hedgehog signaling pathway inhibitor and an antineoplastic agent. It is a member of benzimidazoles, a member of piperidines, a member of phenylureas and a nitrile.
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
Glasdegib Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Suzhou Ryan Pharmachem Technology Co.,Ltd. | +86-512-68780025 +8618962125825 | sales@ryanchem.com | China | 137 | 58 |
| Jinan Carbotang Biotech Co.,Ltd. | +8615866703830 | figo.gao@foxmail.com | China | 7019 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| career henan chemical co | +86-0371-86658258 15093356674; | factory@coreychem.com | China | 29826 | 58 |
| Career Henan Chemica Co | +86-0371-86658258 15093356674; | laboratory@coreychem.com | China | 30255 | 58 |
| NINGBOBENKANGJS PHARMTECHCO., LTD | +8615990591583 15990591583 | CHINA | 2029 | 58 | |
| HANGZHOU CLAP TECHNOLOGY CO.,LTD | 86-571-88216897,88216896 13588875226 | sales@hzclap.com | CHINA | 6313 | 58 |
| ANHUI WITOP BIOTECH CO., LTD | +8615255079626 | eric@witopchemical.com | China | 23556 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 28251 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10523 | 58 |
Related articles
- How to synthesize Glasdegib?
- Glasdegib was approved in 2018 for the treatment of newly diagnosed acute myeloid leukemia (AML) patients at least 75 years of....
- Dec 28，2023
View Lastest Price from Glasdegib manufacturers
| Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
|---|---|---|---|---|---|---|---|---|
 |
2023-05-08 | Glasdegib（PF-04449913）
1095173-27-5
|
US $0.00-0.00 / g | 100g | 98% | kg grade | Suzhou Ryan Pharmachem Technology Co.,Ltd. | |
 |
2020-01-13 | PF-04449913 (Glasdegib)
1095173-27-5
|
US $6.68 / KG | 1KG | 97%-99% | 1kg-1000kg | Career Henan Chemical Co |
-
- Glasdegib（PF-04449913）
1095173-27-5
- US $0.00-0.00 / g
- 98%
- Suzhou Ryan Pharmachem Technology Co.,Ltd.
-
- PF-04449913 (Glasdegib)
1095173-27-5
- US $6.68 / KG
- 97%-99%
- Career Henan Chemical Co