Glasdegib

Product Name: Glasdegib
CAS No.: 1095173-27-5
Chemical Name: Glasdegib
Synonyms: CS-1041;Glasdegib;EOS-60832;PF 04449913;Glasdegib-D3;Glasdegib-D4;Glasdegib-13C6;Glasdegib-13C,15N;Glasdegib USP/EP/BP;PF04449913; PF 04449913
CBNumber: CB82658197
Molecular Formula: C21H22N6O
Formula Weight: 374.44
MOL File: 1095173-27-5.mol

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Glasdegib Property

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
InChI: InChI=1S/C21H22N6O/c1-27-11-10-16(24-21(28)23-15-8-6-14(13-22)7-9-15)12-19(27)20-25-17-4-2-3-5-18(17)26-20/h2-9,16,19H,10-12H2,1H3,(H,25,26)(H2,23,24,28)/t16-,19-/m1/s1
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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H361Suspected of damaging fertility or the unborn child

H373May cause damage to organs through prolonged or repeated exposure

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P281Use personal protective equipment as required.

P308+P313IF exposed or concerned: Get medical advice/attention.

P314Get medical advice/attention if you feel unwell.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 9002936
Product name: PF-04449913
Purity: ≥98%
Packaging: 1mg
Price: $34
Updated: 2024/03/01

Cayman Chemical

Product number: 9002936
Product name: PF-04449913
Purity: ≥98%
Packaging: 5mg
Price: $109
Updated: 2024/03/01

Cayman Chemical

Product number: 9002936
Product name: PF-04449913
Purity: ≥98%
Packaging: 10mg
Price: $198
Updated: 2024/03/01

Cayman Chemical

Product number: 9002936
Product name: PF-04449913
Packaging: 25mg
Price: $412
Updated: 2024/03/01

TRC

Product number: G406550
Product name: Glasdegib
Packaging: 5mg
Price: $135
Updated: 2021/12/16

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Glasdegib Chemical Properties,Usage,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

Raw materials

Preparation Products

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Glasdegib Suppliers

China 110 India 4 United Kingdom 1 United States 15 Global 130

MedChemexpress LLC

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View Lastest Price from Glasdegib manufacturers

Suzhou Ryan Pharmachem Technology Co.,Ltd.

Product: Glasdegib（PF-04449913） 1095173-27-5
Price: US $0.00-0.00/g
Min. Order: 100g
Purity: 98%
Supply Ability: kg grade
Release date: 2023-05-08

Career Henan Chemical Co

Product: PF-04449913 (Glasdegib) 1095173-27-5
Price: US $6.68/KG
Min. Order: 1KG
Purity: 97%-99%
Supply Ability: 1kg-1000kg
Release date: 2020-01-10

1095173-27-5, GlasdegibRelated Search:

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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

PF-04449913 (Glasdegib)

PF04449913; PF 04449913

Urea, N-[(2R,4R)-2-(1H-benzimidazol-2-yl)-1-methyl-4-piperidinyl]-N'-(4-cyanophenyl)-

Glasdegib USP/EP/BP

Glasdegib-13C,15N

Glasdegib-13C6

Glasdegib-D3

Glasdegib-D4

Glasdegib, 10 mM in DMSO

1095173-27-5

Inhibitors