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Purity: ≥98%
Trilaciclib (G-1T28; G1T28; Cosela) is a novel, first-in-class and short-acting CDK4/6 inhibitor approved in 2021 by FDA as a medication to reduce the frequency of chemotherapy-induced bone marrow suppression. It inhibits CDK4/6 at IC50 values of 1 nM and 4 nM, in that order. Preserving hematopoietic stem cells and boosting immune system performance while undergoing chemotherapy are two of its current uses. Treatment outcomes can be markedly improved by administering trilaciclib intravenously before chemotherapy.
| Targets |
CDK4 (IC50 = 1 nM); CDK6 (IC50 = 40 nM)
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| ln Vitro |
G1T28 is a highly effective and specific CDK4/6 inhibitor that prevents RB from being phosphorylated and causes an exclusive, reversible G1 arrest. G1T28 shields RB competent cells from chemotherapy-induced damage (measured by γH2AX) and apoptosis via activation of caspase 3/7 both in vitro and in vivo. [1]
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| ln Vivo |
G1T28 modulates HSPC proliferation in vivo in a dose-and time-dependent manner in both mouse and canine bone marrow. Complete blood counts (CBCs) can recover from chemotherapy more quickly in mice that have received G1T28 pretreatment. Furthermore, rather than shielding RB-deficient tumors from chemotherapy, G1T28 strengthens the anti-tumor effect.[1]
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| Enzyme Assay |
Treatments for HS68, WM2664, and A2058 cells include 300 nM Trilaciclib (G1T28) or DMSO (0.1%) for 4, 8, 16, or 24 hours. Using 1× HALT protease and phosphatase inhibitors in 1× radioimmunoprecipitation assay buffer, whole cell extracts are made. In accordance with the manufacturer's instructions, the kit is used to determine the total protein concentration. Protein is prepared as previously mentioned for Western blot analysis. Antibodies against both total RB and β-tubulin are evaluated as a loading control [1].
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| Cell Assay |
Trilaciclib (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 |
Mice：H69 cells are inserted into female athymic nude mice, who are then watched until treatment starts. When tumors are 150 mm3 in size, mice are given different doses of Trilaciclib (100 mg/kg) and topotecan five days a week for four weeks. Up to 60 days following treatment, tumors are measured. All mice are humanely put to death if their tumor burden reaches an excessive level before 60 days. The amounts of topotecan and trilaciclib in the blood plasma from mice given either topotecan or trilaciclib hydrochloride are processed and examined utilizing accepted techniques.
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| References |
| Molecular Formula |
C24H30N8O
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|---|---|
| Molecular Weight |
446.55
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| Exact Mass |
446.25
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| Elemental Analysis |
C, 64.55; H, 6.77; N, 25.09; O, 3.58
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| CAS # |
1374743-00-6
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| Related CAS # |
Trilaciclib hydrochloride;1977495-97-8
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| Appearance |
White to yellow solid powder
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| LogP |
0.87
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| SMILES |
CN1CCN(CC1)C2=CN=C(C=C2)NC3=NC=C4C=C5C(=O)NCC6(N5C4=N3)CCCCC6
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| InChi Key |
PDGKHKMBHVFCMG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H30N8O/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)
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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
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| Synonyms |
G1T-28; G1T28; G1T 28; Cosela
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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 |
| 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) |
DMSO: 2~6.8 mg/mL (4.5~15.3 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 | 2.2394 mL | 11.1970 mL | 22.3939 mL | |
| 5 mM | 0.4479 mL | 2.2394 mL | 4.4788 mL | |
| 10 mM | 0.2239 mL | 1.1197 mL | 2.2394 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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