Glasdegib [1095173-27-5]
Cat# HY-16391-10mg
Size : 10mg
Brand : MedChemExpress
Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM.
For research use only. We do not sell to patients.
Glasdegib Chemical Structure
CAS No. : 1095173-27-5
This product is a controlled substance and not for sale in your territory.
Based on 4 publication(s) in Google Scholar
Other Forms of Glasdegib:
- Glasdegib maleate Get quote
Description |
Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM[1]. |
IC50 & Target |
IC50: 4 nM (Smo)[1] |
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In Vitro |
Glasdegib (PF-04449913) inhibits sonic hedgehog (Shh) stimulated luciferase expression in mouse embryonic fibroblasts with an IC50 of 6.8 nM; and significantly reduces medulloblastoma growth in a Ptch1+/-p53+/- allograft model at doses that decreased murine Shh target gene expression. In stromal co-culture experiments, FACS analysis demonstrates a significant reduction in BC LSC by Glasdegib (PF-04449913) when compared with normal progenitors. Importantly, human BC LSC engrafted RAG2-/-γC-/- mice treated daily with Glasdegib (PF-04449913) compared with vehicle treated controls have a significant spleen weight reduction (p=0.006). This reduction in leukemic burden corresponded with decreased GLI2 protein expression, as determined by both nanoproteomic analysis of FACS purified human progenitors and GLI2 confocal fluorescence microscopic analysis of splenic sections[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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In Vivo |
Human BC LSC engrafted RAG2-/-γC-/- mice treated daily with Glasdegib (PF-04449913) compared with vehicle treated controls had a significant spleen weight reduction (p=0.006). When 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. These results highlight the important niche dependent effects of selective SMO inhibition that induce GLI2 downregulation in a cell type and context specific manner[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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Molecular Weight |
374.44 |
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Formula |
C21H22N6O |
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CAS No. |
1095173-27-5 |
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Unlabeled CAS |
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Appearance |
Solid |
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Color |
White to off-white |
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SMILES |
O=C(NC1=CC=C(C#N)C=C1)N[C@H]2C[C@H](C3=NC4=CC=CC=C4N3)N(C)CC2 |
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Shipping | Room temperature in continental US; may vary elsewhere. |
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Storage |
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Solvent & Solubility |
In Vitro:
DMSO : 62.5 mg/mL (166.92 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
View the Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume Number of animals Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO
+
%
+
%
Tween-80
+
%
Saline
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
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Purity & Documentation |
Purity: 99.31% |
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References |
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Complete Stock Solution Preparation Table
*
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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DMSO | 1 mM | 2.6707 mL | 13.3533 mL | 26.7066 mL | 66.7666 mL |
5 mM | 0.5341 mL | 2.6707 mL | 5.3413 mL | 13.3533 mL | |
10 mM | 0.2671 mL | 1.3353 mL | 2.6707 mL | 6.6767 mL | |
15 mM | 0.1780 mL | 0.8902 mL | 1.7804 mL | 4.4511 mL | |
20 mM | 0.1335 mL | 0.6677 mL | 1.3353 mL | 3.3383 mL | |
25 mM | 0.1068 mL | 0.5341 mL | 1.0683 mL | 2.6707 mL | |
30 mM | 0.0890 mL | 0.4451 mL | 0.8902 mL | 2.2256 mL | |
40 mM | 0.0668 mL | 0.3338 mL | 0.6677 mL | 1.6692 mL | |
50 mM | 0.0534 mL | 0.2671 mL | 0.5341 mL | 1.3353 mL | |
60 mM | 0.0445 mL | 0.2226 mL | 0.4451 mL | 1.1128 mL | |
80 mM | 0.0334 mL | 0.1669 mL | 0.3338 mL | 0.8346 mL | |
100 mM | 0.0267 mL | 0.1335 mL | 0.2671 mL | 0.6677 mL |