| Identification | Back Directory | [Name]
G1T28 | [CAS]
1977495-97-8 | [Synonyms]
G1T28
Trilaciclib HCl
G1T28 hydrochloride
Trilaciclib hydrochloride
Trilaciclib dihydrochloride
Trilaciclib hydrochloride(G1T28)
2'-[[5-(4-Methylpiperazin-1-yl)pyridin-2-yl]amino}-7',8'-dihydro-6'H-spiro[cyclohexane-1,9'-pyrazino[1',2':1,5]pyrrolo[2,3-d]pyrimidin]-6'-one, hydrochloride (1:2) | [Molecular Formula]
C24H32Cl2N8O | [MDL Number]
MFCD31630829 | [MOL File]
1977495-97-8.mol | [Molecular Weight]
519.47 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
Ethanol: Slightly solublePBS (pH 7.2): Slightly soluble | [form ]
Solid | [color ]
Light yellow to yellow | [Water Solubility ]
Water : ≥ 100 mg/mL (192.50 mM) | [InChIKey]
KZNCPACHGMMKHH-UHFFFAOYSA-N | [SMILES]
O=C1NCC2(CCCCC2)N2C3=NC(NC4N=CC(N5CCN(C)CC5)=CC=4)=NC=C3C=C12.Cl |
| Hazard Information | Back Directory | [Uses]
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]. | [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].
| 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. |
| [IC 50]
Cdk4/cyclin D1: 1 nM (IC50); cdk6/cyclin D3: 4 nM (IC50) | [storage]
Store at -20°C | [References]
[1] Bisi JE, et al. Preclinical Characterization of G1T28: A Novel CDK4/6 Inhibitor for Reduction of Chemotherapy-Induced Myelosuppression. Mol Cancer Ther. 2016 May;15(5):783-93. DOI:10.1158/1535-7163.MCT-15-0775 |
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