2320462-65-3

2320462-65-3 structure

Name: HPK1-IN-7
Chemical Name: HPK1-IN-7
CAS Number: 2320462-65-3
Molecular Formula: C₂₄H₂₂N₆O₄
Molecular Weight: 458.47
Catalog: Signaling Pathways MAPK/ERK Pathway MAP4K
Create Date: 2022-01-10 17:52:46
Modify Date: 2025-09-26 12:24:20
HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1[1].

Name	HPK1-IN-7
Synonyms	1(3H)-Isobenzofuranone, 5-[[4-[[(1S)-2-hydroxy-1-phenylethyl]amino]-5-(1,3,4-oxadiazol-2-yl)-2-pyrimidinyl]amino]-3,3-dimethyl-

Description	HPK1-IN-7 is a potent, orally active HPK1 (hematopoietic progenitor kinase 1, MAP4K1) inhibitor (IC50=2.6 nM) with excellent family and kinome selectivity. HPK1-IN-7 shows selectivity against IRAK4 (59 nM) and GLK (140 nM). HPK1-IN-7 shows robust efficacy against MC38 syngeneic tumor model in combination with anti-PD1[1].
Related Catalog	Signaling Pathways >> MAPK/ERK Pathway >> MAP4K Research Areas >> Cancer
Target	HPK1:2.6 nM (IC50) GLK/MAP4K3:140 nM (IC50) IRAK4:59 nM (IC50) Fms/CSFR:3.2 nM (IC50) FLT3:25.4 nM (IC50) AMPKA1:44.3 nM (IC50) cKIT:45.7 nM (IC50) MST1:55.1 nM (IC50) ICK:65.1 nM (IC50) MST2:78.5 nM (IC50)
In Vivo	HPK1-IN-7 (100 mg/kg; p.o.; twice daily for 28 days) shows robust enhancement of anti-PD1 efficacy in a syngeneic tumor model of colorectal cancer[1]. HPK1-IN-7 (compound 24) (1 mg/kg; intravenous; mice) is characterized by moderate plasma clearance (43 mL/min/kg) and a large volume of distribution (4.4 L/kg). After oral administration (20 mg/kg), the Cmax was 5.3 μM and the AUC0-24h was 19 μM•h. The calculated oral bioavailability based on these pharmacokinetics studies is approximately 100%[1]. Animal Model: Mice (MC38 syngeneic tumor model)[1] Dosage: 100 mg/kg Administration: Oral; twice daily for 28 days Result: Enhanced the efficacy of anti-PD1 treatment, garnering a 100% cure rate vs a 20% cure rate with anti-PD1 alone.
References	[1]. Degnan AP, et al. Discovery of Orally Active Isofuranones as Potent, Selective Inhibitors of Hematopoetic Progenitor Kinase 1. ACS Med Chem Lett. 2021;12(3):443-450. Published 2021 Feb 19.

Molecular Formula	C₂₄H₂₂N₆O₄
Molecular Weight	458.47

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