1. MAPK/ERK Pathway
  2. MAP4K
  3. HPK1-IN-7

HPK1-IN-7 

Cat. No.: HY-138742 Purity: 99.61%
Handling Instructions

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.

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

HPK1-IN-7 Chemical Structure

HPK1-IN-7 Chemical Structure

CAS No. : 2320462-65-3

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5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

IC50 & Target[1]

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].

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

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.
Molecular Weight

458.47

Formula

C₂₄H₂₂N₆O₄

CAS No.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (272.65 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1812 mL 10.9058 mL 21.8117 mL
5 mM 0.4362 mL 2.1812 mL 4.3623 mL
10 mM 0.2181 mL 1.0906 mL 2.1812 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.54 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
HPK1-IN-7
Cat. No.:
HY-138742
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