Description
IACS-13909 is a selective, potent and orally active SHP2 allosteric inhibitor with an IC50 of 15.7 nM and a Kd of 32 nM. IACS-13909 is more selective for SHP2 than other phosphatases (including SHP1). IACS-13909 has antitumor activities and suppresses MAPK pathway signaling in receptor tyrosine kinases (RTK)-dependent cancers.
Product information
CAS Number: 2160546-07-4
Molecular Weight: 377.27
Formula: C17H18Cl2N6
Chemical Name: 1-[3-(2,3-dichlorophenyl)-2H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methylpiperidin-4-amine
Smiles: CC1(N)CCN(CC1)C1C=NC2C(N=1)=NNC=2C1=CC=CC(Cl)=C1Cl
InChiKey: AMADCPJVPLUGQO-UHFFFAOYSA-N
InChi: InChI=1S/C17H18Cl2N6/c1-17(20)5-7-25(8-6-17)12-9-21-15-14(23-24-16(15)22-12)10-3-2-4-11(18)13(10)19/h2-4,9H,5-8,20H2,1H3,(H,22,23,24)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 10 mg/mL (26.51 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
IACS-13909 (10 nM-10 μM; 14 days) treatment potently suppresses the proliferation of wild-type SHP2 and KYSE-520 cells. IACS-13909 (1-5 μM; 2 hours) treatment potently suppresses pERK and pMEK levels in wild-type SHP2 and KYSE-520 cells. IACS-13909 potently suppresses the proliferation of both the parental cells and NCI-H1975 CS cells in a dose-dependent manner, with similar potency (GI50 ~1 μM). IACS-13909 (0.041-3.3 μM) suppresses pERK in NCI-H1975 CS cells in a dose-dependent manner.
In Vivo:
IACS-13909 (70 mg/kg; oral administration; daily; for 21 days) treatment potently suppresses tumor growth in mice, with 100% tumor growth inhibition (TGI) observed following 21 days of dosing.
Products are for research use only. Not for human use.
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