HPK1-IN-31
HPK1-IN-31 (compound 5i) is an orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 value of 0.8 nM. HPK1-IN-31 has anti-tumour activity and has great potential for immunoresearch.
For research use only. We do not sell to patients.
- CAS No.: 3003026-16-9
- Formula: C30H33N7O3
- Molecular Weight:539.63
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All MAP4K Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| T-cell | EC50 |
0.5 μM
Compound: 5i
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Induction of T-cell activation in Balb/c mouse derived anti-CD28-stimulated Pan T cells assessed as increase in IL-2 production incubated for 48 hrs by ELISA
Induction of T-cell activation in Balb/c mouse derived anti-CD28-stimulated Pan T cells assessed as increase in IL-2 production incubated for 48 hrs by ELISA
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[PMID: 36542759] |
| T-cell | IC50 |
>5000 nM
Compound: 5i
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Cytotoxicity against Balb/c mouse derived anti-CD28-stimulated Pan T cells assessed as reduction in cell viability by Cell Titer Glo assay
Cytotoxicity against Balb/c mouse derived anti-CD28-stimulated Pan T cells assessed as reduction in cell viability by Cell Titer Glo assay
|
[PMID: 36542759] |
The pharmacokinetic parameters of HPK1-IN-31(compound 5i)in Mice and Beagles
| mice | beagles | |||
| 5i | 1 mg/kg (i.v.) | 20 mg/kg (i.g.) | 1 mg/kg (i.v.) | 5 mg/kg (i.g.) |
| T1/2 (h) | 1.3 | 3.7 | 8.1 | 6.2 |
| Tmax (h) | - | 0.8 | - | 1.0 |
| Cmax (ng/mL) | 1118 | 2048 | 1811.2 | 539.3 |
| AUC(0-inf)(ng*h/mL) | 860 | 8528 | 3132.2 | 4094.9 |
| MRT (h) | 1.0 | 3.9 | 7.3 | 8.1 |
| CL (mL/min/kg) | 19.7 | - | 5.9 | - |
| F (%) | - | 49 | - | 27 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 3003026-16-9
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Molecular Weight 539.63
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Formula C30H33N7O3
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SMILES
CC(O)(CN1C=C(C=N1)C2=CN=C3N=C2N[C@@H](C4=C(OCCCCC5=CC(N3)=CC=C5C#N)C=CC=C4)CO)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)