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Notch inhibitor 1

Cat. No. M14574
Notch inhibitor 1 Structure
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Biological Activity

Notch inhibitor 1 is a potent Notch inhibitor, with IC50s of 7.8 and 8.5 nM for Notch 1 and Notch 3, respectively. Used in the research of cancer.

Chemical Information
Molecular Weight 574.49
CAS Number 1584647-27-7
Solubility (25°C) DMSO 10 mg/mL
Storage 2-8°C, sealed
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] Juan-Li Duan, et al. Shear stress-induced cellular senescence blunts liver regeneration through Notch-sirtuin 1-P21/P16 axis

[2] Toshihiko Doi, et al. A phase 1 study of crenigacestat (LY3039478), the Notch inhibitor, in Japanese patients with advanced solid tumors

[3] Timothy M Smith Jr, et al. Targeting ADAM10 in Cancer and Autoimmunity

[4] Lijing Cai, et al. Combined antitumor effects of 1,25‑dihydroxy vitamin D3 and Notch inhibitor in liver cancer

[5] Jue Wang, et al. Lingo-1 shRNA and Notch signaling inhibitor DAPT promote differentiation of neural stem/progenitor cells into neurons

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Keywords: Notch inhibitor 1 supplier, Notch, inhibitors, activators

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