HPK1-IN-31

Cat. No.: HY-152257: FAQs
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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.

HPK1-IN-31 Chemical Structure

CAS No. : 3003026-16-9

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Purity & Documentation
References
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Description

In Vivo

HPK1-IN-31(compound 5i) (p.o., 30 or 100 mpk twice daily, 14 days) inhibits tumour growth in the CT26 tumour-bearing female BALB/c mouse model and the MC38 tumour-bearing female C57BL/6 mouse model, and is followed by a significant effect when combined with anti-PD-1 monotherapy^[1].
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.)
T_1/2 (h)	1.3	3.7	8.1	6.2
T_max (h)	-	0.8	-	1.0
C_max (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.

Molecular Weight

539.63

Formula

C₃₀H₃₃N₇O₃

CAS No.

3003026-16-9

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Ming-Shu Wang, et al. Discovery of Macrocycle-Based HPK1 Inhibitors for T-Cell-Based Immunotherapy. J Med Chem. 2023 Jan 12;66(1):611-626. [Content Brief]

HPK1-IN-31 Related Classifications

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Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

HPK1-IN-313003026-16-9MAP4KMAPK Kinase Kinase KinaseHPK1anti-tumourimmunotherapyInhibitorinhibitorinhibit

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