An allosteric inhibitor of SHP-2
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IACS-13909

Item No. 40654

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl]-4-methyl-4-piperidinamine
CAS Number
2160546-07-4
Molecular Formula
C17H18Cl2N6
Formula Weight
377.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly Soluble: 1-10 mg/mlEthanol: Sparingly Soluble: 1-10 mg/ml
SMILES
ClC1=CC=CC(C2=NNC3=NC(N4CCC(C)(CC4)N)=CN=C32)=C1Cl
InChi Code
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)
InChi Key
AMADCPJVPLUGQO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $171

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    10 mg

    $325

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    50 mg

    $598

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    100 mg

    $1,023

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    Cayman Chemical
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    Product Description

    IACS-13909 is an allosteric inhibitor of Src homology region 2 domain-containing phosphatase 2 (SHP-2; IC50 = 11 nM).1 It binds wild-type SHP-2 and SHP-2 containing a constitutively activating glutamate-to-lysine substitution at position 76 (SHP-2E76K; Kds = 49 and 211 nM, respectively). IACS-13909 decreases the levels of phosphorylated ERK in KYSE-520 esophageal squamous cell carcinoma cells (IC50 = 47 nM) but also inhibits human-ether-a-go-go (hERG) channels (IC50 = 180 nM in whole-cell patch-clamp assays using CHO cells). It decreases tumor volume without affecting body weight in an EGFR-overexpressing KYSE-520 mouse xenograft model when administered at a dose of 70 mg/kg per day.2 IACS-13909 (70 mg/kg per day) induces sustained reduction in tumor volume after dosing cessation in a non-small cell lung cancer (NSCLC) mouse xenograft model using H1975 cells expressing drug-resistant EGFRL858R/T790M/C797S.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Czako, B., Sun, Y., McAfoos, T., et al. Discovery of 6-[(3S,4S)-4-amino-3-methyl-2-oxa-8-azaspiro[4.5]decan-8-yl]-3-(2,3-dichlorophenyl)-2-methyl-3,4-dihydropyrimidin-4-one (IACS-15414), a potent and orally bioavailable SHP2 inhibitor. J. Med. CHem. 64(20), 15141-15169 (2021).

    2. Sun, Y., Meyers, B.A., Czako, B., et al. Allosteric SHP2 inhibitor, IACS-13909, overcomes EGFR-dependent and EGFR-independent resistance mechanisms toward osimertinib. Cancer Res. 80(21), 4840-4853 (2020).