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

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

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Trilaciclib Chemical Structure

Trilaciclib Chemical Structure

CAS No. : 1374743-00-6

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Based on 1 publication(s) in Google Scholar

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Trilaciclib Related Antibodies

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1 Publications Citing Use of MCE Trilaciclib

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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Description

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

IC50 & Target

IC50: 1 nM (CDK4), 4 nM (CDK6)[1]
In Vitro

Trilaciclib (10-1000 nM; 24 h) reversibly modulates the proliferation of mouse and canine bone marrow hematopoietic stem and progenitor cells[1].
Trilaciclib (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 (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 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: Produced a strong dose-dependent inhibition of HSPC proliferation within 12 hours.
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).

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

Cell Cycle Analysis[1]

Cell Line: HS68, WM2664 cells
Concentration: 300 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.
In Vivo

Trilaciclib (50-150 mg/kg; po; single dose) protects mouse bone marrow cells from chemotherapy-induced apoptosis and attenuates chemotherapy-induced myelosuppression in vivo. Trilaciclib at 150 mg/kg reduces HSPC damage induced by 5FU (HY-90006) (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

446.55

Formula

C24H30N8O
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

O=C1NCC2(N3C1=CC4=CN=C(NC5=NC=C(N6CCN(C)CC6)C=C5)N=C43)CCCCC2
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 : 6.73 mg/mL (15.07 mM; ultrasonic and warming and adjust pH to 5 with 1 M HCL 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 2.2394 mL 11.1970 mL 22.3939 mL
5 mM 0.4479 mL 2.2394 mL 4.4788 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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Purity & Documentation

Purity: 99.32%

SDS (393 KB)

COA (250 KB) HNMR (147 KB) RP-HPLC (246 KB) LCMS (102 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. 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 2.2394 mL 11.1970 mL 22.3939 mL 55.9848 mL
5 mM 0.4479 mL 2.2394 mL 4.4788 mL 11.1970 mL
10 mM 0.2239 mL 1.1197 mL 2.2394 mL 5.5985 mL
15 mM 0.1493 mL 0.7465 mL 1.4929 mL 3.7323 mL
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Trilaciclib 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:

Trilaciclib1374743-00-6G1T28CDKCyclin dependent kinaseInhibitorinhibitorinhibit

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