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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Protein Phosphatase/PTP-IACS-13909
IACS-13909

Chemical Structure : IACS-13909

CAS No.: 2160546-07-4

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IACS-13909 (IACS13909, IACS 13909)

货号: 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).

规格 价格 库存 数量
5 mg ￥1980 In stock
10 mg ￥2980 In stock
25 mg ￥4880 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 377.273
分子式 C17H18Cl2N6
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

1-(3-(2,3-dichlorophenyl)-1H-pyrazolo[3,4-b]pyrazin-6-yl)-4-methylpiperidin-4-amine

参考文献

1. Yuting Sun, et al. Cancer Res. 2020 Nov 1;80(21):4840-4853.

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