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

Trilaciclib hydrochloride  (Synonyms: G1T28 hydrochloride)

Cat. No.: HY-101467A Purity: 99.74%
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Trilaciclib (G1T28) hydrochloride is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib hydrochloride attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy.

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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Based on 1 publication(s) in Google Scholar

Other Forms of Trilaciclib hydrochloride:

Trilaciclib hydrochloride Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Trilaciclib hydrochloride

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Description

Trilaciclib (G1T28) hydrochloride is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib hydrochloride attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy[1].

IC50 & Target[1]

Cdk4/cyclin D1

1 nM (IC50)

cdk6/cyclin D3

4 nM (IC50)

In Vitro

Trilaciclib hydrochloride (10-1000 nM; 24 h) reversibly modulates the proliferation of mouse and canine bone marrow hematopoietic stem and progenitor cells[1].
Trilaciclib hydrochloride (10-1000 nM; 24 h) can arrest the cell cycle of CDK4/6-dependent cells in the G1 phase, with an EC50 of 30 nM for HS68[1].
Trilaciclib hydrochloride (300 nM; 16 or 48 h) protects CDK4/6 dependent cells (HS68, WM2664) from chemotherapy-induced damage, and attenuates chemotherapy-induced-apoptosis[1].

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

Trilaciclib hydrochloride Related Antibodies

Cell Proliferation Assay[1]

Cell Line: HS68, WM2664 cells
Concentration: 300 nM
Incubation Time: 8h for measure γH2AX foci (DNA damage); 48 hours to measure caspase 3/7 activity (apoptosis).
Result: Elicited a robust dose-dependent decrease in caspase 3/7 activation suggesting an attenuation of apoptosis.
Resulted a dose-dependent decrease in γH2AX foci in all DNA damaging chemotherapies tested (carboplatin, doxorubicin, etoposide, camptothecin).

Cell Cycle Analysis[1]

Cell Line: HS68, WM2664 cells
Concentration: 10, 30, 100, 300, 1000 nM
Incubation Time: 24 h
Result: Inhibited only CDK4/6-dependent cells, with EC50 of 30 nM for HS68 cell.
Singnificantly decreased the S phase cell numbers, increased the G1 phase cell numbers.

Western Blot Analysis[1]

Cell Line: HS68, WM2664 cells
Concentration: 10, 30, 100, 300, 1000 nM
Incubation Time: 16 h
Result: Blocked RB phosphorylation in the RB dependent cell lines by 16 hours post exposure, while the CDK4/6-independent cell line (A2058) exhibits no RB or pRB expression. Suggesting an attenuation of chemotherapy-induced DNA damag
In Vivo

Trilaciclib hydrochloride (50-150 mg/kg; po; single dose) protects mouse bone marrow cells from chemotherapy-induced apoptosis and attenuates chemotherapy-induced myelosuppression in vivo. Trilaciclib hydrochloride at 150 mg/kg reduces HSPC damage induced by 5FU (150 mg/kg; ip) chemotherapy, thereby accelerating blood count recovery after chemotherapy[1].

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

Animal Model: FVB/n female C57Bl6 mice[1]
Dosage: 50, 100, 150 mg/kg
Administration: Po; single dose; treated followed 11 or 23 hours later by a single injection of EdU (HY-118411) (100 μg; ip); mouse were euthanized 1 hour after EdU injection.
Result: Showed a dose-dependent decrease in caspase 3/7 activation.
Attenuated chemotherapy-induced myelosuppression in mice.
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.

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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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(per animal)

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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%

COA (248 KB) HNMR (273 KB) LCMS (254 KB)

Handling Instructions (2659 KB)
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

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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.

Keywords:

Trilaciclib1977495-97-8G1T28CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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