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IACS-13909

Cat. No. M10738
IACS-13909  Structure
Size Price Availability Quantity
5mg USD 285  USD285 In stock
10mg USD 450  USD450 In stock
25mg USD 890  USD890 In stock
50mg USD 1340  USD1340 In stock
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Quality Control & Documentation
Biological Activity

IACS-13909 is a potent selective, orally active SHP2 allosteric inhibitor IC50 for 15.7 nM,Kd 32 nM. IACS-13909 is more selective for SHP2 than other phosphatase, including SHP1. IACS-13909 inhibits the signaling of the receptor tyrosine kinase (RTK)/MAPK pathway and has an anticancer effect.

Chemical Information
Molecular Weight 377.27
Formula C17H18Cl2N6
CAS Number 2160546-07-4
Form Solid
Solubility (25°C) DMSO ≥ 10 mg/mL
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] Yuting Sun, et al. Cancer Res. Allosteric SHP2 Inhibitor, IACS-13909, Overcomes EGFR-Dependent and EGFR-Independent Resistance Mechanisms toward Osimertinib

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  Catalog
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Keywords: IACS-13909 supplier, Phosphatase, inhibitors, activators


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