HPK1-IN-55
HPK1-IN-55 (compound 19) is a selective and orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 of <0.51 nM. HPK1-IN-55 shows excellent kinase selectivity (>637-fold vs GCK-like kinase and >1022-fold vs LCK). HPK1-IN-55 has anticancer effects.
For research use only. We do not sell to patients.
- CAS No.: 3048537-58-9
- Formula: C30H34N8O3
- Molecular Weight:554.64
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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HPK1 <0.51 nM (IC50) |
HPK1-IN-55 (0.5-10000 nM, 5 h) demonstrates HPK1 enzymatic inhibition with an IC50 of <0.51 nM and inhibits IL-2 secretion with an EC50 of 43.3 nM in human PBMCs [1].
HPK1-IN-55 (0.001-100 nM) stimulates IL-2 and IFN-γ release with EC50 values of 38.8 and 49.2 nM, respectively in purified human pan T cells[1].
HPK1-IN-55 (0.00457-10 μM, 72 h) increases T cell proliferation at low, intermediate and high concentrations in human pan T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human pan T cells
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Concentration:0.00457, 0.01372, 0.04115, 0.12346, 0.37037, 1.11111, 3.33333, 10 μM
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Incubation Time:72 h
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Result:Increased T cell proliferation at low, intermediate and high concentrations in human pan T cells.
HPK1-IN-55 (1 mg/kg, i.v., 2 mg/kg, p.o.) exhibits moderate clearance (Clp = 11.41mL/min/kg) as well as good oral exposure (DNAUC(0−24h) = 560.5 h•ng/mL) and bioavailability (F % = 42.0) in monkeys[1].
HPK1-IN-55 (1.5-12 mg/kg, p.o., b.i.d, 5 weeks) exhibits good target engagement in the CT26 model[1].
In Vivo Pharmacokinetics of HPK1-IN-55 .
| HPK1-IN-55 | ||
| beagle dogs IV | Clp (mL/min/kg) Vd (L/kg) |
11.44 5.58 |
| beagle dogs PO | DNAUC (0-24 h) (h・ng/ml) t1/2 (h) F (%) |
563 7.65 41.5 |
| cyno monkeys IV | Clp (mL/min/kg) Vd (L/kg) |
11.41 5.07 |
| cyno monkeys PO | DNAUC (0-24 h) (h・ng/ml) t1/2 (h) F (%) |
560.5 8.73 42 |
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