Pimicotinib hydrochloride  (Synonyms: ABSK021 hydrochloride)

Pimicotinib (ABSK021) hydrochloride is a selective CSF1R inhibitor with an IC₅₀ value of 19.48 nM (determined by inhibiting ADP production). Pimicotinib hydrochloride exhibits anti-tumor activity^[1][2][3].

Pimicotinib hydrochloride has IC₅₀ values of 76.98 nM and 1399.21 nM for the KIT and PDGFRA kinases^[1].
Pimicotinib hydrochloride can strongly inhibit the phosphorylation of CSF1R and the proliferation of bone-marrow-derived macrophages at low nanomolar concentrations^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pimicotinib hydrochloride has anti-tumor activity in NCI-H2122 PBMC humanized mice and LLC syngeneic mice. It shows a better effect when used in combination with Sotorasib (HY-114277). It can lead to a reduction in the number of immunosuppressive tumor-associated macrophages, an enhancement of the regulatory effect of the tumor microenvironment related to anti-tumor immunity, and more infiltration of CD8 T cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

456.93

C₂₂H₂₅ClN₆O₃

2866305-19-1

O=C(N1C(C(C)(CC1)C)=O)NC2=CC=C(OC3=CC=NC(C4=CN(C)N=C4)=C3)C(C)=N2.Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Zhao BW, et al. N-(azaaryl)cyclolactam-1-carboxamide derivative, preparation method and application. World Intellectual Property Organization, WO2018214867 A1. 2018-11-29.

  [2]. Yang S, et al. Abstract LB-288: A highly selective small molecule CSF-1R inhibitor demonstrates strong immunomodulatory activity in syngeneic models. Cancer Research, 2018, 78(13_Supplement): LB-288-LB-288.

  [3]. Zhang N, et al. Abstract LB077: CSF-1R inhibition with Pimicotinib (ABSK021) enhanced anti-tumor efficacy of KRASG12C inhibitors in preclinical non-small cell lung cancer mouse models. Cancer Research, 2024, 84(7_Supplement): LB077-LB077.