1. Cell Cycle/DNA Damage
  2. CDK
  3. Trilaciclib hydrochloride

Trilaciclib hydrochloride  (Synonyms: G1T28 hydrochloride)

Cat. No.: HY-101467A Purity: 99.74%
COA Handling Instructions

Trilaciclib hydrochloride (G1T28 hydrochloride) is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively.

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

Trilaciclib hydrochloride Chemical Structure

Trilaciclib hydrochloride Chemical Structure

CAS No. : 1977495-97-8

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1 mg USD 40 In-stock
5 mg USD 110 In-stock
10 mg USD 200 In-stock
50 mg USD 700 In-stock
100 mg USD 1120 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Trilaciclib hydrochloride:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Trilaciclib hydrochloride

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Trilaciclib hydrochloride (G1T28 hydrochloride) is a CDK4/6 inhibitor with IC50s of 1 nM and 4 nM for CDK4 and CDK6, respectively[1].

IC50 & Target[1]

Cdk4/cyclin D1

1 nM (IC50)

cdk6/cyclin D3

4 nM (IC50)

In Vitro

Incubation with Trilaciclib hydrochloride (G1T28) for 24 hours induces a robust G1 cell-cycle arrest (time=0). By 16 hours after Trilaciclib hydrochloride washout, cells have reentered the cell cycle and demonstrate cell-cycle kinetics similar to untreated control cells. These results demonstrate that Trilaciclib hydrochloride causes a transient, and reversible G1 arrest. A transient Trilaciclib hydrochloride-mediated G1 cell-cycle arrest in CDK4/6-sensitive cells decreases the in vitro toxicity of a variety of commonly used cytotoxic chemotherapy agents associated with myelosuppression[1].

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

In Vivo

Trilaciclib hydrochloride (G1T28) treatment results in a robust and dose-dependent suppression of proliferation in HSPCs at 12 hours, with 5-ethynyl-2′-deoxyuridine (EdU) incorporation returning near baseline levels in a dose-dependent manner by 24 hours after administration. These data demonstrate that a single oral dose of Trilaciclib hydrochloride can produce reversible cell-cycle arrest in HSPCs in a dose-dependent manner in vivo. Mice given 100 mg/kg Trilaciclib hydrochloride 30 minutes prior to etoposide treatment, exhibits only background levels of caspase-3/7 activity. These data demonstrate that Trilaciclib hydrochloride can protect the bone marrow from chemotherapy-induced apoptosis in vivo. The data demonstrate that treatment with Trilaciclib hydrochloride prior to 5-fluorouracil (5-FU) likely decreases 5-FU-induced damage by chemotherapy in HSPCs, thus accelerating blood count recovery after chemotherapy[1].

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

Clinical Trial
Molecular Weight

519.47

Formula

C24H32Cl2N8O

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=CC3=CN=C(NC4=CC=C(N5CCN(C)CC5)C=N4)N=C3N2C6(CCCCC6)CN1.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 25.64 mg/mL (49.36 mM; ultrasonic and adjust pH to 2 with HCl)

DMSO : 1.1 mg/mL (2.12 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 1.9250 mL 9.6252 mL 19.2504 mL
5 mM 0.3850 mL 1.9250 mL 3.8501 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

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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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.74%

References
Kinase Assay
[1]

HS68, WM2664, and A2058 cells are treated with 300 nM Trilaciclib hydrochloride (G1T28) or DMSO (0.1%), for 4, 8, 16, or 24 hours. Whole cell extracts are prepared using 1× radioimmunoprecipitation assay buffer containing 1× HALT protease and phosphatase inhibitors. Total protein concentration is determined by using the kit, according to the manufacturer's instructions. For Western blot analysis, protein is processed as described previously. Antibodies to total RB and β-tubulin run as a loading control are assessed[1].

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

Cell Assay
[1]

HS68 cells are treated for 24 hours with Trilaciclib hydrochloride (G1T28) at 10, 30, 100, 300, 1,000, or 3,000 nM final concentration. Cells are harvested and fixed in ice-cold methanol. Fixed cells are stained with 20 μg propidium iodide, 50 μg RNAse A in PBS-CMF (calcium magnesium free) +1% BSA, Fraction V. Samples are processed on Cyan ADP Analyzer, and cell-cycle analysis is completed using software[1].

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

Animal Administration
[1]

Female athymic nude mice are implanted with H69 cells and monitored until treatment initiation. Once tumors reach an acceptable size (150 mm3), mice are dosed in various combinations of Trilaciclib hydrochloride (G1T28) and topotecan for 5 days per week for 4 weeks. Tumors are measured for up to 60 days after treatment. All mice that reach excessive tumor burden before 60 days are humanely euthanized. Topotecan and Trilaciclib hydrochloride levels in blood plasma from the mice treated with Trilaciclib hydrochloride and/or topotecan are processed and analyzed using established methods[1].

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

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 (sealed storage, away from moisture). 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 / H2O 1 mM 1.9250 mL 9.6252 mL 19.2504 mL 48.1260 mL
H2O 5 mM 0.3850 mL 1.9250 mL 3.8501 mL 9.6252 mL
10 mM 0.1925 mL 0.9625 mL 1.9250 mL 4.8126 mL
15 mM 0.1283 mL 0.6417 mL 1.2834 mL 3.2084 mL
20 mM 0.0963 mL 0.4813 mL 0.9625 mL 2.4063 mL
25 mM 0.0770 mL 0.3850 mL 0.7700 mL 1.9250 mL
30 mM 0.0642 mL 0.3208 mL 0.6417 mL 1.6042 mL
40 mM 0.0481 mL 0.2406 mL 0.4813 mL 1.2031 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Trilaciclib hydrochloride 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.

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Trilaciclib hydrochloride
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