[CAS NO. 1374743-00-6] Trilaciclib

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PRODUCTS SPECIFICATIONS [1374743-00-6]

Catalog

AS963826

Brand

Arctom Scientific

CAS

1374743-00-6

DESCRIPTION [1374743-00-6]

Overview

MDL	-
Molecular Weight	446.55
Molecular Formula	C24H30N8O
SMILES	O=C1NCC2(N3C1=CC4=CN=C(NC5=NC=C(N6CCN(C)CC6)C=C5)N=C43)CCCCC2

For research use only. We do not sell to patients.

1 Publications Citing Use of MCE

[1]Department of Biochemistry. 2020 Oct.

Summary

Trilaciclib is a CDK4/6 inhibitor with IC ₅₀ s of 1 nM and 4 nM for CDK4 and CDK6 , respectively.

IC50 & Target

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

In Vitro

Incubation with Trilaciclib (G1T28) for 24 hours induces a robust G ₁ cell-cycle arrest (time=0). By 16 hours after Trilaciclib hydrochloride washout, cells have reentered the cell cycle and demonstrate cell-cycle kinetics similar to untreated control cells. These results demonstrate that Trilaciclib causes a transient, and reversible G ₁ arrest. A transient Trilaciclib-mediated G ₁ cell-cycle arrest in CDK4/6-sensitive cells decreases the in vitro toxicity of a variety of commonly used cytotoxic chemotherapy agents associated with myelosuppression ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Trilaciclib (G1T28) treatment results in a robust and dose-dependent suppression of proliferation in HSPCs at 12 hours, with EdU incorporation returning near baseline levels in a dose-dependent manner by 24 hours after administration. These data demonstrate that a single oral dose of Trilaciclib can produce reversible cell-cycle arrest in HSPCs in a dose-dependent manner in vivo . Mice given 100 mg/kg Trilaciclib 30 minutes prior to etoposide treatment, exhibits only background levels of caspase-3/7 activity. These data demonstrate that Trilaciclib can protect the bone marrow from chemotherapy-induced apoptosis in vivo . The data demonstrate that treatment with Trilaciclib prior to 5-FU likely decreases 5-FU-induced damage by chemotherapy in HSPCs, thus accelerating blood count recovery after chemotherapy ^[1] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT04902885	Jiangsu Simcere Pharmaceutical Co., Ltd.\|G1 Therapeutics, Inc.	Extensive-stage Small-cell Lung Cancer	May 25, 2021	Phase 3
NCT03041311	G1 Therapeutics, Inc.\|Roche-Genentech	Small Cell Lung Cancer	June 29, 2017	Phase 2
NCT02978716	G1 Therapeutics, Inc.	Triple-Negative Breast Neoplasms\|Breast Neoplasm\|Breast Cancer\|Triple-Negative Breast Cancer	February 2, 2017	Phase 2
NCT04607668	G1 Therapeutics, Inc.	Colorectal Cancer Metastatic\|Myelosuppression-Adult\|Chemotherapeutic Toxicity	October 16, 2020	Phase 3
NCT01042379	QuantumLeap Healthcare Collaborative	Breast Neoplasms\|Breast Cancer\|Breast Tumors\|Angiosarcoma\|TNBC - Triple-Negative Breast Cancer\|HER2-positive Breast Cancer\|HER2-negative Breast Cancer\|Hormone Receptor Positive Tumor\|Hormone Receptor Negative Tumor\|Early-stage Breast Cancer\|Locally Advanced Breast Cancer	March 1, 2010	Phase 2
NCT05071703	Jiangsu Simcere Pharmaceutical Co., Ltd.\|G1 Therapeutics, Inc.	Extensive-stage Small-cell Lung Cancer	June 2, 2021	Phase 4
NCT05578326	UNC Lineberger Comprehensive Cancer Center\|G1 Therapeutics, Inc.	Lung Cancer\|Small-cell Lung Cancer	October 12, 2022	Phase 2
NCT05113966	G1 Therapeutics, Inc.	Triple Negative Breast Cancer	November 22, 2021	Phase 2
NCT04799249	G1 Therapeutics, Inc.	TNBC - Triple-Negative Breast Cancer\|Breast Cancer	April 15, 2021	Phase 3
NCT04863248	G1 Therapeutics, Inc.	Metastatic Non-Small Cell Lung Cancer\|NSCLC\|Lung Cancer	April 16, 2021	Phase 2
NCT04504513	G1 Therapeutics, Inc.\|Bionical Emas	Myelosuppression Adult\|Chemotherapeutic Toxicity\|Small Cell Lung Cancer
NCT02499770	G1 Therapeutics, Inc.	Small Cell Lung Cancer	June 26, 2015	Phase 1\|Phase 2
NCT04887831	G1 Therapeutics, Inc.	Urothelial Carcinoma\|Bladder Cancer\|Myelosuppression Adult\|Chemotherapy-induced Neutropenia\|Metastatic Bladder Cancer	June 4, 2021	Phase 2
NCT05112536	G1 Therapeutics, Inc.	Triple Negative Breast Cancer\|Breast Cancer	November 19, 2021	Phase 2
NCT02514447	G1 Therapeutics, Inc.	Small Cell Lung Cancer	October 5, 2015	Phase 1\|Phase 2

Appearance

Solid

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 : 6.82 mg/mL ( 15.27 mM ; ultrasonic and adjust pH to 6 with HCl)

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
10 mM	0.2239 mL	1.1197 mL	2.2394 mL

* Please refer to the solubility information to select the appropriate solvent.

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.