Art. -Nr.: HY-157149

DS21150768

Name: DS21150768
Brand: MedChemExpress
SKU: HY-157149
Price: 610.00 USD
Availability: InStock
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DS21150768 is an orally active HPK1 inhibitor with an IC₅₀ of 3.27 nM against hHPK1. DS21150768 decreases pSLP76 levels and increases IL-2 levels. DS21150768 shows antitumor effects in multiple syngeneic mouse tumor models, and in combination with anti-PD-1 antibody enhances antitumor efficacy in multiple models. DS21150768 induces immune-related gene signatures in responsive tumor models.

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Reinheit : 99.16%
CAS. Nr.: 3074816-62-6
Formel: C₃₆H₃₂F₂N₆O₂
Molecular Weight:618.68

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

DS21150768 Chemical Structure

CAS. Nr.: 3074816-62-6

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

HY-138742
HPK1-IN-7

HPK1 Inhibitor

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]

HPK1

3.27 nM (IC₅₀)

IL-2

Alle MAP4K Isoform-spezifische Produkte anzeigen :

Alle Interleukin Related Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Jurkat	IC50	61.9 nM	Inhibition of anti-CD3/CD28-induced SLP76 phosphorylation in human Jurkat Clone E6-1 cells incubated 24 hrs then stimulated 60 mins, measured by AlphaLISA SureFire Ultra p-SLP-76 (Ser376) assay. Inhibition of anti-CD3/CD28-induced SLP76 phosphorylation in human Jurkat Clone E6-1 cells incubated 24 hrs then stimulated 60 mins, measured by AlphaLISA SureFire Ultra p-SLP-76 (Ser376) assay.	37944847

In Vitro

Adaptive ImmunityCytokines & ChemokinesImmune Tolerance & ImmunosuppressionCytokines and ChemokinesOthers

Adaptive Immunity

Cytokines & Chemokines

Immune Tolerance & Immunosuppression

DS21150768 (4 days) combined with anti-PD-L1 antibody augments IFN-γ secretion in mouse allogeneic mixed lymphocyte reaction^[1].

Adaptive Immunity

Cytokines and Chemokines

DS21150768 (30 min-24 h) inhibits anti-CD3/CD28-induced SLP76 phosphorylation in Jurkat cells with an IC₅₀ of 61.9 nM and enhances IL-2 secretion^[1].
DS21150768 (16 h) promotes IL-2 production from anti-CD3-stimulated mouse splenocytes in the presence of PGE2, NECA, or TGF-β^[1].

Others

DS21150768 (0.15-2,5000 nM; 30 min) inhibits recombinant human HPK1 kinase activity with an IC₅₀ of 3.27 nM under 1 mM ATP^[1].
DS21150768 (32-20,000 nM) binds human HPK1 with a K_D of 6.08 nM and a dissociation half-life of 722 min^[1].
DS21150768 (200 nM) inhibits 10 of 174 tested kinases by >50% and shows no >20% inhibition among highlighted TCR pathway kinases^[1].
DS21150768 (0.1 μM; 4 h) exhibits >99.8% protein binding in male BALB/c mouse serum^[1].

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

In Vivo

Adaptive ImmunityCytokines and ChemokinesAnti-cancerImmune Tolerance & Immunosuppression

Adaptive Immunity

Cytokines and Chemokines

DS21150768 (30-100 mg/kg; oral; single administration) reduces splenic pSLP76 levels in mice and enhances IL-2 and IFN-γ production after TCR stimulation in vivo, and the enhancement of plasma IFN-γ is completely abolished in HPK1-KO mice^[1].

Anti-cancer

Immune Tolerance & Immunosuppression

DS21150768 (100 mg/kg; oral; once every 2 days) alone produces 10% tumor growth inhibition in the A20 syngeneic tumor mouse model, and in combination with an anti-PD-1 antibody produces 20% tumor growth inhibition^[1].
DS21150768 (100 mg/kg; oral; once every 2 days) alone produces 38% tumor growth inhibition in the B16-BL6 syngeneic tumor mouse model, and in combination with an anti-PD-1 antibody produces 29% tumor growth inhibition^[1].
DS21150768 (100 mg/kg; oral; once every 2 days), both alone and in combination with an anti-PD-1 antibody, produces 18% tumor growth inhibition in the B16-F10 syngeneic tumor mouse model^[1].
DS21150768 (100 mg/kg; oral; once every 2 days) alone produces 44% tumor growth inhibition in the CT26.WT syngeneic tumor mouse model, and in combination with an anti-PD-1 antibody produces 67% tumor growth inhibition^[1].
DS21150768 (100 mg/kg; oral; once every 2 days) alone produces 33% tumor growth inhibition in the EMT6 syngeneic tumor mouse model, and in combination with an anti-PD-1 antibody produces 90% tumor growth inhibition^[1].
DS21150768 (100 mg/kg; oral; once every 2 days) alone produces 21% tumor growth inhibition in the H22 syngeneic tumor mouse model, and in combination with an anti-PD-1 antibody produces 80% tumor growth inhibition^[1].
DS21150768 (100 mg/kg; oral; once every 2 days) alone produces 36% tumor growth inhibition in the RM-1 syngeneic tumor model, and in combination with an anti-PD-1 antibody produces 43% tumor growth inhibition^[1].

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

Animal Model:

C57BL/6JJcl; HPK1-knockout (HPK1-KO) mice with a C57BL/6J background^[1]
Dosage:

30 mg/kg; 100 mg/kg
Administration:

p.o.; single dose
Result:

At 30 and 100 mg/kg, splenic pSLP76 was substantially reduced after 24 h, and suppression was maintained for 48 h.
At 30 mg/kg, IFN-γ was elevated in plasma and spleen.
At 100 mg/kg, both IL-2 and IFN-γ were increased.
The enhancement of plasma IFN-γ level was completely abrogated in HPK1-KO mice.

Animal Model:

BALB/c^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once every 2 days
Result:

Tumor growth inhibition (TGI) at endpoint for monotherapy was 10%.
Tumor growth inhibition (TGI) at endpoint for the combination with anti-PD-1 antibody was 20%.

Animal Model:

C57BL/6^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once every 2 days
Result:

Tumor growth inhibition (TGI) at endpoint for monotherapy was 38%.
Monotherapy significantly inhibited tumor growth.
Tumor growth inhibition (TGI) at endpoint for the combination with anti-PD-1 antibody was 29%.

Animal Model:

C57BL/6^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once every 2 days
Result:

Tumor growth inhibition (TGI) at endpoint for monotherapy was 18%.
Tumor growth inhibition (TGI) at endpoint for the combination with anti-PD-1 antibody was 18%.

Animal Model:

BALB/c^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once every 2 days
Result:

Tumor growth inhibition (TGI) at endpoint for monotherapy was 44%.
Monotherapy significantly inhibited tumor growth.
Tumor growth inhibition (TGI) at endpoint for the combination with anti-PD-1 antibody was 67%.

Animal Model:

BALB/c^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once every 2 days
Result:

Tumor growth inhibition (TGI) at endpoint for monotherapy was 33%.
Tumor growth inhibition (TGI) at endpoint for the combination with anti-PD-1 antibody was 90%.

Animal Model:

BALB/c^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once every 2 days
Result:

Tumor growth inhibition (TGI) at endpoint for monotherapy was 21%.
Tumor growth inhibition (TGI) at endpoint for the combination with anti-PD-1 antibody was 80%.

Animal Model:

C57BL/6^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once every 2 days
Result:

Tumor growth inhibition (TGI) at endpoint for monotherapy was 12%.
Tumor growth inhibition (TGI) at endpoint for the combination with anti-PD-1 antibody was 80%.

Animal Model:

C57BL/6^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once every 2 days
Result:

Tumor growth inhibition (TGI) at endpoint for monotherapy was 13%.
Tumor growth inhibition (TGI) at endpoint for the combination with anti-PD-1 antibody was 19%.

Animal Model:

C57BL/6^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once every 2 days
Result:

Tumor growth inhibition (TGI) at endpoint for monotherapy was 38%.
Monotherapy significantly inhibited tumor growth.
Tumor growth inhibition (TGI) at endpoint for the combination with anti-PD-1 antibody was 80%.

Animal Model:

C57BL/6^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once every 2 days
Result:

Tumor growth inhibition (TGI) at endpoint for monotherapy was 60%.
Monotherapy significantly inhibited tumor growth.
Tumor growth inhibition (TGI) at endpoint for the combination with anti-PD-1 antibody was 81%.

Animal Model:

BALB/c^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once every 2 days
Result:

Tumor growth inhibition (TGI) at endpoint for monotherapy was 44%.
Monotherapy significantly inhibited tumor growth.
Tumor growth inhibition (TGI) at endpoint for the combination with anti-PD-1 antibody was 50%.

Animal Model:

C57BL/6^[1]
Dosage:

100 mg/kg
Administration:

p.o.; once every 2 days
Result:

Tumor growth inhibition (TGI) at endpoint for monotherapy was 36%.
Monotherapy significantly inhibited tumor growth.
Tumor growth inhibition (TGI) at endpoint for the combination with anti-PD-1 antibody was 43%.

Related Protocols :

Patient-Derived Xenograft (PDX)

Chemical Information

CAS. Nr. 3074816-62-6
Appearance Solid
Molecular Weight 618.68
Formel C₃₆H₃₂F₂N₆O₂
Color Off-white to light yellow
SMILES

FC1=CC=C(N2C(C(C(NC3=CC=C(C4=C(N)N=CC(C5=CC(C)=NC(C)=C5)=C4)C=C3)=O)=C(NCC6(C7)CC7(F)C6)C=C2)=O)C=C1
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (161.63 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.6163 mL

8.0817 mL

16.1634 mL

5 mM

0.3233 mL

1.6163 mL

3.2327 mL

10 mM

0.1616 mL

0.8082 mL

1.6163 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.04 mM); Suspended solution

This protocol yields a suspended solution of ≥ 2.5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.04 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (290 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

Verweise

[1]. Setsu G, et al. Highly potent, orally active novel small-molecule HPK1 inhibitor DS21150768 induces anti-tumor responses in multiple syngeneic tumor mouse models. European journal of pharmacology. 2023 Dec 15;961:176184. [Content Brief]

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.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6163 mL	8.0817 mL	16.1634 mL	40.4086 mL
	5 mM	0.3233 mL	1.6163 mL	3.2327 mL	8.0817 mL
	10 mM	0.1616 mL	0.8082 mL	1.6163 mL	4.0409 mL
	15 mM	0.1078 mL	0.5388 mL	1.0776 mL	2.6939 mL
	20 mM	0.0808 mL	0.4041 mL	0.8082 mL	2.0204 mL
	25 mM	0.0647 mL	0.3233 mL	0.6465 mL	1.6163 mL
	30 mM	0.0539 mL	0.2694 mL	0.5388 mL	1.3470 mL
	40 mM	0.0404 mL	0.2020 mL	0.4041 mL	1.0102 mL
	50 mM	0.0323 mL	0.1616 mL	0.3233 mL	0.8082 mL
	60 mM	0.0269 mL	0.1347 mL	0.2694 mL	0.6735 mL
	80 mM	0.0202 mL	0.1010 mL	0.2020 mL	0.5051 mL
	100 mM	0.0162 mL	0.0808 mL	0.1616 mL	0.4041 mL

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DS21150768

Alle MAP4K Isoform-spezifische Produkte anzeigen

Alle Interleukin Related Isoform-spezifische Produkte anzeigen