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Cat. No.: HY-168110

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HPK1-IN-52

HPK1-IN-52 is a potent and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC₅₀ value of 10.4 nM. HPK1-IN-52 exhibits anti-tumor activities.

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

CAS No.: 2994298-66-5
Formula: C₃₁H₃₀F₂N₆O₂
Molecular Weight:556.61

Storage:

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

Data Sheet (276 KB)

HPK1-IN-52 Chemical Structure

CAS No.: 2994298-66-5

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Protocols (1)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

HPK1-IN-52 is a potent and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC₅₀ value of 10.4 nM. HPK1-IN-52 exhibits anti-tumor activities^[1].

IC₅₀ & Target

^[1]

HPK1

10.4 nM (IC₅₀)

MAP4K2

448 nM (IC₅₀)

GLK/MAP4K3

85 nM (IC₅₀)

MAP4K4

665 nM (IC₅₀)

MAP4K5

104 nM (IC₅₀)

MAP4K6

168 nM (IC₅₀)

All MAP4K Isoforms :

In Vitro

HPK1-IN-52 (compound 24) shows comparable activity (IC₅₀ of 10.4 nM) and cellular potency (pSLP76 EC₅₀ of 41 nM & IL-2 EC₅₀ of 108 nM)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.

In Vivo

HPK1-IN-52 (compound 24; 30 mg/kg; po; twice daily; for two weeks) exhibits moderate tumor-growth inhibition (TGI) of 42%^[1].
HPK1-IN-52's plasma clearance significantly improved (Cl_p = 46 mL/min/kg) in mice, and its oral exposure dramatically increased (AUC_(0–24h) = 4139 h ng/mL). In addition, HPK1-IN-52 exhibits lower in vivo clearance (Cl_p = 67 mL/min/kg) and higher oral exposure (AUC_(0–24h) = 2013 h ng/mL) in rats^[1].

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

Animal Model:

Balb/c mice injected with CT26 cells^[1]
Dosage:

30 mg/kg
Administration:

po; twice daily; for two weeks
Result:

Exhibited moderate tumor-growth inhibition.

Chemical Information

CAS No. 2994298-66-5
Molecular Weight 556.61
Formula C₃₁H₃₀F₂N₆O₂
SMILES

O=C1NC=CC2=C1C(NC3=NC(CN4C[C@@H](F)CC4)=C(C5CCOCC5)C=C3)=CC=C2C6=CN=C7C=C(F)C=CN76
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

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

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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]. Jingjing Peng, et al. Discovery of 1(2H)-phthalazinone and 1(2H)-isoquinolinone derivatives as potent hematopoietic progenitor kinase 1 (HPK1) inhibitors. European Journal of Medicinal Chemistry. Volume 279, 5 December 2024, 116877.

Calculators

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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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MOQ

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100 mg

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