Lerociclib(G1T38) (C008B-271086)

G1T38 (Lerociclib) is a novel, potent, selective, and orally bioavailableCDK4/6inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively.TargetsCDK4 (Cell-free assay); CDK6 (Cell-free assay); CDK9 (Cell-free assay) 1 nM; 2 nM; 28 nMIn vitroG1T38 is highly potent and selective for CDK4/cyclin D1 and CDK6/cyclin D3 over CDK1, CDK2, CDK5 and CDK7 and their respective binding partners. G1T38 decreases RB1 (RB) phosphorylation, causes a precise G1 arrest, and inhibits cell proliferation in a variety of CDK4/6-dependent tumorigenic cell lines including breast, melanoma, leukemia, and lymphoma cells with EC50 concentrations as low as 23 nM.In vivoG1T38 treatment leads to equivalent or improved tumor efficacy compared to the first-in-class CDK4/6 inhibitor, palbociclib, in an ER+ breast cancer xenograft model. Furthermore, G1T38 accumulates in mouse xenograft tumors but not plasma, resulting in less inhibition of mouse myeloid progenitors than after palbociclib treatment. In larger mammals, this difference in pharmacokinetics allows for 28 day continuous dosing of G1T38 in beagle dogs without producing severe neutropenia.Cell Research(from reference)Cell lines：WM2664 cells Concentrations：300 nM Incubation Time：1, 4, 8, 16, and 24 hours

CDK9 Selective Inhibitors

Specifications & Purity: G1T38 (Lerociclib) is a novel, potent, selective, and orally bioavailableCDK4/6inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively.TargetsCDK4 (Cell-free assay); CDK6 (Cell-free assay); CDK9 (Cell-free assay) 1 nM; 2 nM; 28 nMIn vitroG1T38 is highly potent and selective for CDK4/cyclin D1 and CDK6/cyclin D3 over CDK1, CDK2, CDK5 and CDK7 and their respective binding partners. G1T38 decreases RB1 (RB) phosphorylation, causes a precise G1 arrest, and inhibits cell proliferation in a variety of CDK4/6-dependent tumorigenic cell lines including breast, melanoma, leukemia, and lymphoma cells with EC50 concentrations as low as 23 nM.In vivoG1T38 treatment leads to equivalent or improved tumor efficacy compared to the first-in-class CDK4/6 inhibitor, palbociclib, in an ER+ breast cancer xenograft model. Furthermore, G1T38 accumulates in mouse xenograft tumors but not plasma, resulting in less inhibition of mouse myeloid progenitors than after palbociclib treatment. In larger mammals, this difference in pharmacokinetics allows for 28 day continuous dosing of G1T38 in beagle dogs without producing severe neutropenia.Cell Research(from reference)Cell lines：WM2664 cells Concentrations：300 nM Incubation Time：1, 4, 8, 16, and 24 hours

Grade: Moligand™

Molecular Formula: C26H34N8O

Molecular Weight: 474.60

PubChem CID: 86269224

Isomeric SMILES: CC(C)N1CCN(CC1)C2=CN=C(C=C2)NC3=NC=C4C=C5C(=O)NCC6(N5C4=N3)CCCCC6

Storage Temperature: Store at -20°C

Shipped in: Ice chest + Ice pads

UPC:

51292806

Weight:

1.06 Ounces

HazmatClass:

Yes

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

G414063-100mg

Country of Origin:

China

CAS:

1628256-23-4

Product Size:

100mg

Harmonized Tariff Code:

2931.90.90