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SHP2-D26 

Cat. No. M29659
SHP2-D26  Structure
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Biological Activity

SHP2-D26 is a first, potent and effective SHP2 degrader. SHP2-D26 induces SHP2 degradation requires binding to VHL-1 and SHP2 proteins. SHP2-D26 is also neddylation- and proteasome-dependent.

Chemical Information
Molecular Weight 1115.89
Formula C56H79ClN12O6S2
CAS Number 2458219-65-1
Form Solid
Solubility (25°C) DMSO 83.33 mg/mL (ultrasonic)
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] Yunfu Deng, et al. Cancer Gene Ther. Correction to: Therapeutic efficacy of the novel SHP2 degrader SHP2-D26, alone or in combination, against lung cancer is associated with modulation of p70S6K/S6, Bim and Mcl-1

[2] Yunfu Deng, et al. Cancer Gene Ther. Therapeutic efficacy of the novel SHP2 degrader SHP2-D26, alone or in combination, against lung cancer is associated with modulation of p70S6K/S6, Bim and Mcl-1

[3] Mingliang Wang, et al. J Med Chem. Correction to "Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein"

[4] Kai Tang, et al. Eur J Med Chem. Medicinal chemistry strategies for the development of protein tyrosine phosphatase SHP2 inhibitors and PROTAC degraders

[5] Mingliang Wang, et al. J Med Chem. Discovery of SHP2-D26 as a First, Potent, and Effective PROTAC Degrader of SHP2 Protein

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  Catalog
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Keywords: SHP2-D26  supplier, Phosphatase, inhibitors, activators


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