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MedChemExpress - Model Trilaciclib ...

MedChemExpress - Model Trilaciclib hydrochloride - 1977495-97-8

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].

Trilaciclib hydrochloride

MCE China：Trilaciclib hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-101467A

CAS：1977495-97-8

Synonyms：G1T28 hydrochloride

Purity：99.69%

Storage：4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

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.

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].

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].

IC50 & Target：Cdk4/cyclin D1 1 nM (IC50) cdk6/cyclin D3 4 nM (IC50)

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. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。