2. MAPK/ERK Pathway Immunology/Inflammation
  3. MAP4K Interleukin Related
  4. AZ3246

AZ3246 is an orally active and selective inhibitor of HPK1 with an IC50 of < 3 nM. AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM. AZ3246 is a low-clearance antitumor compound that can be used for the study of breast cancer.

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AZ3246

AZ3246 Chemical Structure

CAS No. : 2893978-54-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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AZ3246 Related Antibodies

Top Publications Citing Use of Products

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MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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Description

AZ3246 is an orally active and selective inhibitor of HPK1 with an IC50 of < 3 nM. AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM. AZ3246 is a low-clearance antitumor compound that can be used for the study of breast cancer[1].

In Vitro

AZ3246 (100 nM) is highly selective for HPK1 over STK3, STK4, and TNIK , hits only HPK1 and MYLK at >80% inhibition, hits ROS1, YSK4 and TNIK at >50% inhibition[1].
AZ3246 has excellent metabolic stability in human liver microsomes[1].
AZ3246 induces IL-2 secretion in T cells with an EC50 of 90 nM without inhibiting antagonistic kinases[1].
AZ3246 exhibits low CLint values in primary human, rat, and dog hepatocytes. Low turnover was also observed in HμREL cocultures for rat, dog, monkey, and human hepatocytes[1].

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

AZ3246 Related Antibodies
In Vivo

AZ3246 (30 mg/kg; p.o.; twice daily) inhibits tumor growth in EMT6 mouse model, AZ3246 (30-150 mg/kg) shows no effect on animal bodyweight [1].
AZ3246 (10-100 mg/kg; p.o.) exposure in mouse is linear up to 30 mg/kg with a limited increase in exposure at 100 mg/kg[1].
AZ3246 is a low-clearance compound, consistent with a neutral molecule that is not heavily metabolized by the liver[1].

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

Animal Model: Female Balb/c mice with EMT6 cells injected subcutaneously into the right flank[1]
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); twice daily
Result: Inhibited tumor growth and similar to that of a monotherapy of 10 mg/kg murine anti-PD-L1 antibody (twice weekly)
Animal Model: Female Balb/c mice with EMT6 cells injected subcutaneously into the right flank[1]
Dosage: 30 mg/kg
Administration: Oral gavage (p.o.); twice daily
Result: Inhibited tumor growth and similar to that of a monotherapy of 10 mg/kg murine anti-PD-L1 antibody (twice weekly).
Molecular Weight

471.44

Formula

C21H20F3N9O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

FC(F)(CN1N=C(C)C(NC2=C(C(N)=O)N=C(C3=CN=CC4=C3N=CN4C)C(C5CC5)=N2)=C1)F
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (106.06 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1212 mL 10.6058 mL 21.2116 mL
5 mM 0.4242 mL 2.1212 mL 4.2423 mL
View the Complete Stock Solution Preparation Table

* 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.

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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1212 mL 10.6058 mL 21.2116 mL 53.0290 mL
5 mM 0.4242 mL 2.1212 mL 4.2423 mL 10.6058 mL
10 mM 0.2121 mL 1.0606 mL 2.1212 mL 5.3029 mL
15 mM 0.1414 mL 0.7071 mL 1.4141 mL 3.5353 mL
20 mM 0.1061 mL 0.5303 mL 1.0606 mL 2.6515 mL
25 mM 0.0848 mL 0.4242 mL 0.8485 mL 2.1212 mL
30 mM 0.0707 mL 0.3535 mL 0.7071 mL 1.7676 mL
40 mM 0.0530 mL 0.2651 mL 0.5303 mL 1.3257 mL
50 mM 0.0424 mL 0.2121 mL 0.4242 mL 1.0606 mL
60 mM 0.0354 mL 0.1768 mL 0.3535 mL 0.8838 mL
80 mM 0.0265 mL 0.1326 mL 0.2651 mL 0.6629 mL
100 mM 0.0212 mL 0.1061 mL 0.2121 mL 0.5303 mL
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AZ3246 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:

AZ32462893978-54-4AZ 3246AZ-3246MAP4KInterleukin RelatedMAPK Kinase Kinase KinaseILAnticancerHPK1 inhibitorIL-2Inhibitorinhibitorinhibit

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