HPK1-IN-40-d₂

Cat. No.: HY-149773S: FAQs
Data Sheet Handling Instructions

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HPK1-IN-40 (compound 49) is a potent and selective HPK1 inhibitor with an IC₅₀ of 0.9 nM. HPK1-IN-40 reinvigorates T-cell receptor (TCR) signaling, promoting T-cell function and cytokine production in T cells while having anti-cancer activity.

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

HPK1-IN-40-d<sub>2</sub> Chemical Structure

HPK1-IN-40-d₂ Chemical Structure

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Purity & Documentation
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Description

IC₅₀ & Target

HPK1^[1]IC₅₀: 0.9 nM^[1]

In Vitro

HPK1-IN-40 (0.1 μM, 1 μM) improves the IL-2 secretion of Jurkat cells , leads to augmented T cell function^[1].
HPK1-IN-40 (0.03 μM ~ 1 μM )inhibits the HPK1 signaling in T cells^[1].
1.19
Pharmacokinetic Parameters of HPK1-IN-40 in Rats^[1]

Route	Parameter	Rat (1 mg/kg)
IV	T_1/2(h)	0.898
	AUC_last(h*ng/mL)	355
	V_ss(L/kg)	2.45
	Cl_hep (mL/min/kg)	46.8
Route	Parameter	Rat (3 mg/kg)
PO	T_1/2 (h)	0.499
	T_max (h)	0.250
	AUC_last(h*ng/mL)	1.91
	C_max (ng/mL)	3.62
	F%	0.179

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

Western Blot Analysis^[1]

Cell Line:	Jurkat, primary mouse T cells
Concentration:	0.03, 0.1, 0.3, 1 (μM)
Incubation Time:	1h
Result:	Inhibited the HPK1 signaling in T cells.

In Vivo

HPK1-IN-40 alone (25 mg/kg; i.p.; bid for 7 days) in CT26 tumor-bearing mice causes T cell activation^[1].
HPK1-IN-40 (25 mg/kg; i.p.; bid for 10 days) combines with anti-PD1 antibody (10 mg/kg; i.p.; bid for 10 days) shows synergistic antitumor effects, the CT26 tumor growth rate of HPK1-IN-40 combined with anti-PD1 antibody is the lowest. No significant body weight loss was observed, indicative of good tolerance of the treatment ^[1].

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

Animal Model:	CT26 Tumor-bearing mice
Dosage:	25 mg/kg
Administration:	Twice a day by intraperitoneal injection (i.p.), bid for 7 days.
Result:	Increased IFN-γ⁺CD3⁺ T in CD3⁺ TIL, IFN-γ⁺CD8⁺ T in CD8⁺ TIL, Th1 in CD4⁺ TIL, CD69⁺CD3⁺ T in CD3⁺ TIL, CD69⁺CD8⁺ T in CD8⁺ TIL, CD69⁺CD4⁺ T in CD4⁺ TIL.

Animal Model:	CT26 Tumor-bearing mice
Dosage:	HPK1-IN-40 (25 mg/kg), anti-PD1 antibody (10 mg/kg)
Administration:	HPK1-IN-40 alone / anti-PD1 antibody alone (every 3 days), or the combination treatment, twice a day by intraperitoneal injection (i.p.) for 10 days.
Result:	Showed marginal tumor growth inhibition (TGI = 19.6%). The CT26 tumor growth rate of HPK1-IN-40 combined with anti-PD1 antibody was the lowest, then anti-PD1 alone, then HPK1-IN-40. No significant body weight loss was observed.

Molecular Weight

477.49

Formula

C₂₄H₂₀D₂FN₇O₃

SMILES

OC([2H])([C@@H](NC1=NC(NC2=CC(C(C)(N3)C)=C(C=C2)C3=O)=NC=C1C4=NN=CO4)C5=CC=C(C=C5)F)[2H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

Dissolved in 2.5% DMSO, 5% HS 15, 22.5% poly(ethylene glycol) 400, and 70% physiological saline.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Jing Ai, et al. Design, Synthesis, and Pharmacological Evaluation of Isoindoline Analogues as New HPK1 Inhibitors. Journal of Medicinal Chemistry. 2023，Article ASAP. [Content Brief]

HPK1-IN-40-d₂ Related Classifications

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-40-d₂MAP4KMAPK Kinase Kinase KinaseJurkat cellsCT-26colon tumor modelcancerTMEHPK1Inhibitorinhibitorinhibit

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HPK1-IN-40-d2

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