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HPK1-IN-7

  Cat. No.:  DC46921   Featured
Chemical Structure
2320462-65-3
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More than 5000 active chemicals with high quality for research!
Field of application
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.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 2320462-65-3
Chemical Name: HPK1-IN-7
SMILES: OC[C@@H](NC1=NC(NC2=CC(C3(C)C)=C(C(O3)=O)C=C2)=NC=C1C4=NN=CO4)C5=CC=CC=C5
Formula: C24H22N6O4
M.Wt: 458.480
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
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].
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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
Cat. No. Product name Field of application
DC74333 BAY-405 BAY-405 is a potent and selective MAP4K1 inhibitor with IC50 of 6 nM. BAY-405 potentiates in vitro and in vivo antitumor T-cell reactivity which overcomes the suppression by TGFβ and PGE2.
DC72741 BGB 15025 BGB-15025 is a potent and selective HPK1 inhibitor. It is used in the treatment of various cancers.
DC46921 HPK1-IN-7 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.
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