HPK1-IN-7 structure
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Common Name | HPK1-IN-7 | ||
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CAS Number | 2320462-65-3 | Molecular Weight | 458.47 | |
Density | N/A | Boiling Point | N/A | |
Molecular Formula | C24H22N6O4 | Melting Point | N/A | |
MSDS | N/A | Flash Point | N/A |
Use of HPK1-IN-7HPK1-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 |
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Synonym | More Synonyms |
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]. |
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Related Catalog | |
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 |
Molecular Formula | C24H22N6O4 |
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Molecular Weight | 458.47 |
1(3H)-Isobenzofuranone, 5-[[4-[[(1S)-2-hydroxy-1-phenylethyl]amino]-5-(1,3,4-oxadiazol-2-yl)-2-pyrimidinyl]amino]-3,3-dimethyl- |