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Saridegib

Cat. No. M10835
Saridegib Structure
Synonym:

IPI-926

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Biological Activity

Saridegib is a specific and effective inhibitor of Smo, a key transmembrane signaling protein in the Hedgehog pathway.

Chemical Information
Molecular Weight 504.77
Formula C29H48N2O3S
CAS Number 1037210-93-7
Solubility (25°C) N/A
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Terenzio Cosio, et al. Int J Mol Sci. Patidegib in Dermatology: A Current Review

[2] Verline Justilien, et al. Clin Cancer Res. Molecular pathways: novel approaches for improved therapeutic targeting of Hedgehog signaling in cancer stem cells

[3] Selvarajan Sandhiya, et al. J Pharmacol Pharmacother. The dawn of hedgehog inhibitors: Vismodegib

[4] Michelle J Lee, et al. Proc Natl Acad Sci U S A. Hedgehog pathway inhibitor saridegib (IPI-926) increases lifespan in a mouse medulloblastoma model

[5] Kenneth P Olive, et al. Science. Inhibition of Hedgehog signaling enhances delivery of chemotherapy in a mouse model of pancreatic cancer

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MRT-81 is a potent antagonist of human and rodent smoothened (Smo) receptors, with an IC50 value of 41 nM in the Shh-light2 cells. MRT-81 has potent hedgehog inhibiting activity. MRT-81 can be used for the research of cancer.

Fluticasone

Fluticasone is a corticosteroid and Smo agonist with an IC50 of 99 nM, which activates the Hedgehog signaling pathway and promotes the proliferation of primary neural stem or precursor cells, and can be used in respiratory related studies.

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PF-5274857 hydrochloride 

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Keywords: Saridegib, IPI-926 supplier, Smo, inhibitors, activators


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