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Chemical Structure : IACS-13909
CAS No.: 2160546-07-4
Catalog No.: PC-38070Not For Human Use, Lab Use Only.
IACS-13909 (IACS13909) is a potent, and selective allosteric inhibitor of SHP2 with IC50 of 15.7 nM (hSHP2 full length), Kd of 32 nM (ITC).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $198 | In stock | |
| 10 mg | $298 | In stock | |
| 25 mg | $488 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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IACS-13909 (IACS13909) is a potent, and selective allosteric inhibitor of SHP2 with IC50 of 15.7 nM (hSHP2 full length), Kd of 32 nM (ITC).
IACS-13909 potently suppresses the phosphatase activity of purified full-length, recombinant human SHP2 protein with an IC50 of 15.7 nM.
IACS-13909 does not suppress SHP2 phosphatase activity at 10 uM, acts outside the phosphatase domain.
IACS-13909 displays no inhibitory activity against a panel of 22 phosphatases, and no inhibition of full-length SHP1.
IACS-13909 inhibits the proliferation and MAPK pathway signaling of tumor cell lines driven by a broad spectrum of RTKs in vitro (GI50<100 nM, DK-MG (EGFR vIII+), BV-173 (BCR-ABL), KG-1 (OP2-FGFR1), KU812 (BCR-ABL), SW-13 (ERBB4-IKZF2) and MV-4-11 (FLT3-ITD)).
IACS-13909 inhibits the proliferation and MAPK pathway signaling in RTK-activated cancer cells in vitro due to on-target SHP2 inhibition.
IACS-13909 demonstrates antitumor activity in tumors harboring EGFR-dependent resistance mutation in vitro and in vivo.
| M.Wt | 377.273 | |
| Formula | C17H18Cl2N6 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
1-(3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-4-methylpiperidin-4-amine |
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1. Yuting Sun, et al. Cancer Res. 2020 Nov 1;80(21):4840-4853.
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