1. GPCR/G Protein MAPK/ERK Pathway
  2. Ras
  3. ZT-12-037-01

ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM.

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ZT-12-037-01 Chemical Structure

ZT-12-037-01 Chemical Structure

CAS No. : 2328073-61-4

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Description

ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM[1].

In Vitro

ZT-12-037-01 (3 μM; 14 days) significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation and proliferation[1].
ZT-12-037-01 (0-3 μM) has an inhibitory effects of ZT-12-037-01 on STK19WT and STK19D89N-activated NRAS phosphorylation in HPMs[1].

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

Cell Proliferation Assay[1]

Cell Line: CDK4 (R24C) melanocyte cells; hTERT melanocyte cells; p53DD melanocyte cells
Concentration: 3 μM
Incubation Time: 14 days
Result: Inhibited melanocyte proliferation.

Western Blot Analysis[1]

Cell Line: STK19WT and STK19D89N
Concentration: 0 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time:
Result: Inhibited NRAS phosphorylation.
In Vivo

ZT-12-037-01 (intraperitoneally injection; 25-50 mg/kg; once daily; 21 days) inhibits growth of SK-MEL-2 xenograft melanoma and the sections of tumors indicates induction of apoptosis by increasing cleaved caspase-3[1].

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

Animal Model: SK-MEL-2 xenograft melanoma nude mice with hTERT/p53DD/CDK4(R24C) melanocytes[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: Intraperitoneally injection; 21 days; once a day
Result: Inhibited growth of SK-MEL-2 xenograft melanoma.
Molecular Weight

385.50

Formula

C21H31N5O2

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COC1=CC2=NC(NC3CC3)=NC(NC4CCN(C(C)C)CC4)=C2C=C1OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

1M HCl : 100 mg/mL (259.40 mM; Need ultrasonic)

DMSO : 50 mg/mL (129.70 mM; ultrasonic and adjust pH to 2 with 1M HCl; 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 2.5940 mL 12.9702 mL 25.9403 mL
5 mM 0.5188 mL 2.5940 mL 5.1881 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 5 mg/mL (12.97 mM); Suspended solution; Need ultrasonic

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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / 1M HCl 1 mM 2.5940 mL 12.9702 mL 25.9403 mL 64.8508 mL
5 mM 0.5188 mL 2.5940 mL 5.1881 mL 12.9702 mL
10 mM 0.2594 mL 1.2970 mL 2.5940 mL 6.4851 mL
15 mM 0.1729 mL 0.8647 mL 1.7294 mL 4.3234 mL
20 mM 0.1297 mL 0.6485 mL 1.2970 mL 3.2425 mL
25 mM 0.1038 mL 0.5188 mL 1.0376 mL 2.5940 mL
30 mM 0.0865 mL 0.4323 mL 0.8647 mL 2.1617 mL
40 mM 0.0649 mL 0.3243 mL 0.6485 mL 1.6213 mL
50 mM 0.0519 mL 0.2594 mL 0.5188 mL 1.2970 mL
60 mM 0.0432 mL 0.2162 mL 0.4323 mL 1.0808 mL
80 mM 0.0324 mL 0.1621 mL 0.3243 mL 0.8106 mL
100 mM 0.0259 mL 0.1297 mL 0.2594 mL 0.6485 mL
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  • 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.

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Product Name:
ZT-12-037-01
Cat. No.:
HY-122866
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