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Purity: ≥98%
Trilaciclib hydrochloride (G-1T28; Cosela), the hydrochloride salt of Trilaciclib, is a short-acting CDK4/6 inhibitor with anticancer activity. With IC50s of 1 nM and 4 nM, respectively, it inhibits CDK4/6. FDA approved triadaclib in 2021 as a myelopreservation medication to lessen the incidence of bone marrow suppression brought on by chemotherapy.
| Targets |
Cdk4/cyclin D1 (IC50 = 1 nM); cdk6/cyclin D3 (IC50 = 4 nM)
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| ln Vitro |
A robust G1 cell-cycle arrest (time=0) is induced by incubating with Trilaciclib hydrochloride (G1T28) for 24 hours. At 16 hours following the washout of Trilaciclib hydrochloride, the cells have returned to the cell cycle and exhibit cell-cycle kinetics that are comparable to those of the untreated control group. These findings highlight the transient and reversible G1 arrest caused by triadaceticlib hydrochloride. Numerous widely used cytotoxic chemotherapy agents linked to myelosuppression are less toxic in vitro when Trilaciclib hydrochloride-mediated G1 cell-cycle arrest occurs in CDK4/6-sensitive cells[1].
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| ln Vivo |
After 12 hours of treatment with tilacilib hydrochloride (G1T28), HSPC proliferation is robustly and dose-dependently suppressed. By the 24th hour, 5-ethynyl-2′-deoxyuridine (EdU) incorporation has returned to levels close to baseline in a dose-dependent manner. These findings show that a single oral dosage of trilaciclib hydrochloride can cause a dose-dependent, reversible cell-cycle arrest in HSPCs. Thirty minutes before receiving etoposide treatment, mice given 100 mg/kg of trilaciclib hydrochloride showed only background levels of caspase-3/7 activity. These findings show that trilaciclib hydrochloride can shield bone marrow from apoptosis brought on by chemotherapy in vivo. According to the data, treating HSPCs with trilaciclib hydrochloride before 5-fluorouracil (5-FU) probably reduces the damage that 5-FU causes during chemotherapy, hastening the recovery of blood counts[1].
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| Enzyme Assay |
Treatment of HS68, WM2664, and A2058 cells is performed for 4, 8, 16, or 24 hours with either DMSO (0.1%) or 300 nM Trilaciclib hydrochloride (G1T28). In order to prepare whole cell extracts, 1× HALT protease and phosphatase inhibitors are added to 1× radioimmunoprecipitation assay buffer. By using the kit and following the manufacturer's instructions, one can determine the total protein concentration. Protein is processed as mentioned earlier in order to prepare it for Western blot analysis. As a loading control, antibodies against total RB and β-tubulin are measured[1].
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| Cell Assay |
Trilaciclib hydrochloride (G1T28) at final concentrations of 10, 30, 100, 300, 1,000, or 3,000 nM is applied to HS68 cells for a duration of 24 hours. After harvesting, cells are preserved in ice-cold methanol. PBS-CMF (calcium magnesium free) + 1% BSA, Fraction V, 20 μg propidium iodide, and 50 μg RNAse A are used to stain fixed cells. Software is used to finish the cell-cycle analysis after samples are processed on a Cyan ADP Analyzer[1].
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| Animal Protocol |
After implanting H69 cells, female athymic nude mice are observed until the start of treatment. When the tumors are large enough (150 mm3), mice are given different doses of topotecan and trilaciclib hydrochloride (G1T28) five days a week for four weeks. A maximum of 60 days following treatment are spent measuring tumors. If a mouse's tumor burden becomes too great before 60 days, it is humanely put down. Utilizing established procedures, the levels of topotecan and Trilaciclib hydrochloride in the blood plasma from mice treated with either or both of these agents are processed and examined[1].
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| References |
| Molecular Formula |
C24H32CL2N8O
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|---|---|
| Molecular Weight |
519.469882011414
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| Exact Mass |
518.21
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| Elemental Analysis |
C, 55.49; H, 6.21; Cl, 13.65; N, 21.57; O, 3.08
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| CAS # |
1977495-97-8
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| Related CAS # |
Trilaciclib;1374743-00-6
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| Appearance |
Light yellow to yellow solid powder
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| tPSA |
91.2Ų
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| SMILES |
CN1CCN(CC1)C2=CN=C(C=C2)NC3=NC=C4C=C5C(=O)NCC6(N5C4=N3)CCCCC6.Cl.Cl
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| InChi Key |
BRCYOXKEDFAUSA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H30N8O.2ClH/c1-30-9-11-31(12-10-30)18-5-6-20(25-15-18)28-23-26-14-17-13-19-22(33)27-16-24(7-3-2-4-8-24)32(19)21(17)29-23;;/h5-6,13-15H,2-4,7-12,16H2,1H3,(H,27,33)(H,25,26,28,29);2*1H
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| Chemical Name |
4-[[5-(4-methylpiperazin-1-yl)pyridin-2-yl]amino]spiro[1,3,5,11-tetrazatricyclo[7.4.0.02,7]trideca-2,4,6,8-tetraene-13,1'-cyclohexane]-10-one;dihydrochloride
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| Synonyms |
Trilaciclib hydrochloride; Trilaciclib HCl; G1T-28 hydrochloride; G1T28 HCl; G1T 28 HCl
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ~25.6 mg/mL (~49.4 mM)
DMSO: ~1.1 mg/mL (~2.1 mM) |
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 | |
| 10 mM | 0.1925 mL | 0.9625 mL | 1.9250 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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