1. Metabolic Enzyme/Protease
  2. Ser/Thr Protease
  3. HZ1

Anticancer agent 241 (HZ1) is an orally active first-in-class cyclin-dependent kinase like 3 (CDKL3)-specific inhibitor. Anticancer agent 241 shows a strong tumor-suppressing effect, and has the potential to overcome the resistance of CDK4/6 inhibitor.

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

HZ1 Chemical Structure

HZ1 Chemical Structure

CAS No. : 3030492-40-8

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Based on 1 publication(s) in Google Scholar

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Description

Anticancer agent 241 (HZ1) is an orally active first-in-class cyclin-dependent kinase like 3 (CDKL3)-specific inhibitor. Anticancer agent 241 shows a strong tumor-suppressing effect, and has the potential to overcome the resistance of CDK4/6 inhibitor[1].

In Vitro

Anticancer agent 241 (HZ1; 2-10 h; 100 nM) markedly decreases the levels of pRb and CDK4 hence effectively triggering cell cycle arrest and tumor death[1].

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

Western Blot Analysis[1]

Cell Line: DLD-1 cells
Concentration: 100 nM
Incubation Time: 2 h, 4 h, 6 h, 8 h, 10 h
Result: Reduced the levels of pRb and CDK4.
In Vivo

Anticancer agent 241 (HZ1; 1 mg/kg; oral gavage; daily for 12-14 days) has anticancer activity in a mouse model of colon cancer[1].

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

Animal Model: 6-week-old female athymic nude mice injected with DLD-1 cells[1]
Dosage: 1 mg/kg
Administration: Oral gavage; daily for 12-14 days
Result: Suppressed tumor volume in a mouse model of colon cancer.
Molecular Weight

362.43

Formula

C20H22N6O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C)C(C=C1)=CC=C1NC2=NC(NC3=CC(C4CCCC4)=NN3)=CC=N2

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 (137.96 mM; Need ultrasonic; 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 2.7592 mL 13.7958 mL 27.5915 mL
5 mM 0.5518 mL 2.7592 mL 5.5183 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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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 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, 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 2.7592 mL 13.7958 mL 27.5915 mL 68.9788 mL
5 mM 0.5518 mL 2.7592 mL 5.5183 mL 13.7958 mL
10 mM 0.2759 mL 1.3796 mL 2.7592 mL 6.8979 mL
15 mM 0.1839 mL 0.9197 mL 1.8394 mL 4.5986 mL
20 mM 0.1380 mL 0.6898 mL 1.3796 mL 3.4489 mL
25 mM 0.1104 mL 0.5518 mL 1.1037 mL 2.7592 mL
30 mM 0.0920 mL 0.4599 mL 0.9197 mL 2.2993 mL
40 mM 0.0690 mL 0.3449 mL 0.6898 mL 1.7245 mL
50 mM 0.0552 mL 0.2759 mL 0.5518 mL 1.3796 mL
60 mM 0.0460 mL 0.2299 mL 0.4599 mL 1.1496 mL
80 mM 0.0345 mL 0.1724 mL 0.3449 mL 0.8622 mL
100 mM 0.0276 mL 0.1380 mL 0.2759 mL 0.6898 mL
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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.

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Product Name:
HZ1
Cat. No.:
HY-161847
Quantity:
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