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Cat. No.: HY-153920A

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Pimicotinib hydrochloride

(Synonyms: ABSK021 hydrochloride)

Pimicotinib (ABSK021) hydrochloride is a selective and orally active CSF1R inhibitor with an IC₅₀ value of 19.48 nM (determined by inhibiting ADP production). Pimicotinib hydrochloride exhibits anti-tumor activity.

For research use only. We do not sell to patients.

CAS No.: 2866305-19-1
Formula: C₂₂H₂₅ClN₆O₃
Molecular Weight:456.93

Storage:

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

Data Sheet (268 KB)

Pimicotinib hydrochloride Chemical Structure

CAS No.: 2866305-19-1

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

All PDGFR Isoforms :

In Vitro

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.

In Vivo

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 2866305-19-1
Molecular Weight 456.93
Formula C₂₂H₂₅ClN₆O₃
SMILES

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

ABSK021 hydrochloride
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[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.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Purity & Documentation
References

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Pimicotinib hydrochloride

All PDGFR Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

Pimicotinib hydrochloride Related Classifications

HY-153920A Related Classifications