Glasdegib (PF-04449913)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 100mg | $900 | Check With Us |
| 500mg | $2450 | Check With Us |
| 1g | $3675 | Check With Us |
: Cat #: V1339 CAS #: 1095173-27-5 Purity ≥ 98%
Description: Glasdegib (formerly known as PF-04449913; PF4449913; PF04449913; PF-4449913; Daurismo) is a novel, potent, and orally bioavailable small-molecule inhibitor of Smoothened (Smo) in the Hedgehog (Hh) signaling pathway with potential antitumor activity.
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| Molecular Weight (MW) | 374.44 |
|---|---|
| Molecular Formula | C21H22N6O |
| CAS No. | 1095173-27-5 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 47 mg/mL (125.5 mM)r |
| Water:<1 mg/mLr | |
| Ethanol:<1 mg/mL | |
| SMILES Code | O=C(NC1=CC=C(C#N)C=C1)N[C@H]2C[C@H](C3=NC4=CC=CC=C4N3)N(C)CC2 |
| Synonyms | PF 04449913; PF-4449913; PF-04449913; PF4449913; PF04449913; PF 4449913; daurismo |
| Protocol | 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 |
|---|---|---|
| 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 |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.6707 mL | 13.3533 mL | 26.7065 mL | 53.4131 mL |
| 5mM | 0.5341 mL | 2.6707 mL | 5.3413 mL | 10.6826 mL |
| 10mM | 0.2671 mL | 1.3353 mL | 2.6707 mL | 5.3413 mL |
| 20mM | 0.1335 mL | 0.6677 mL | 1.3353 mL | 2.6707 mL |
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Step Two: Enter the in vivo formulation
%DMSO
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%ddH2O
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Method for preparing DMSO master liquid:
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Method for preparing in vivo formulation:
Take
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DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.