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Lerociclib

Catalog No.: 204302
Cas No.: 1628256-23-4 (free base)
Purity : 98%

Lerociclib , also known as G1T38, is an oral, potent and selective CDK4/6 inhibitor for the treatment of Rb competent tumors. Biochemical profiling demonstrates G1T38 is a competitive, nanomolar inhibitor of CDK4/6 with highly selectivity for CDK4-cyclin D1 and CDK6-cyclin D3. G1T38 exhibits a low EC50>3 μM in Rb null cells. In vivo, daily oral treatment with G1T38 causes significant, durable growth inhibition of tumors in a HER2/neu GEMM and in MCF7 xenograft breast cancer models.

Lerociclib HCl (G1T38 HCl) may be provided. 

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

Chemical Information

NameLerociclib
Iupac Chemical Name2'-((5-(4-isopropylpiperazin-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
SynonymsG1T38; G1T-38; G1T 38; G1-T38; G1 T-38; G1 T38; Lerociclib
Molecular FormulaC26H34N8O
Molecular Weight 474.613
SmileCC(C)N(CC1)CCN1C(C=N2)=CC=C2NC3=NC=C4C(N(C5(CCCCC5)CNC6=O)C6=C4)=N3
InChiKeyYPJRHEKCFKOVRT-UHFFFAOYSA-N
InChi InChI=1S/C26H34N8O/c1-18(2)32-10-12-33(13-11-32)20-6-7-22(27-16-20)30-25-28-15-19-14-21-24(35)29-17-26(8-4-3-5-9-26)34(21)23(19)31-25/h6-7,14-16,18H,3-5,8-13,17H2,1-2H3,(H,29,35)(H,27,28,30,31)
CAS Number1628256-23-4 (free base)
Related CAS2097938-59-3 (HCl) ; 1628256-23-4 (free base)

Ordering Information

PackagingPriceAvailabilityPurityShipping Time
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FormulationPale yellow solid
Purity98%
Storage0 - 4 C for short term (days to weeks), or -20 C for long term (months).
SolubilitySoluble in DMSO
HandlingAvoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation.
Shipping ConditionShipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
HS Code2933999701
TargetsCDK4/6 inhibitor
MechanismLerociclib (G1T38 ) is a novel, selective,differentiated oral CDK4/6 inhibitor with biochemical IC50 values of 1 nM, 2 nM and 28 μnM for CDK4, CDK6 and CDK9 respectively. Lerociclib (G1T38) with potential use in combination with other targeted therapies in certain types of breast and lung cancer.
Cell study
Animal study
Clinical study

1: Bisi JE, Sorrentino JA, Jordan JL, Darr DD, Roberts PJ, Tavares FX, Strum JC. Preclinical development of G1T38: A novel, potent and selective inhibitor ofcyclin dependent kinases 4/6 for use as an oral antineoplastic in patients with CDK4/6 sensitive tumors. Oncotarget. 2017 Mar 15. doi: 10.18632/oncotarget.16216. [Epub ahead of print] PubMed PMID: 28418845.

2: Stice JP, Wardell SE, Norris JD, Yllanes AP, Alley HM, Haney VO, White HS, Safi R, Winter PS, Cocce KJ, Kishton RJ, Lawrence SA, Strum JC, McDonnell DP. CDK4/6 Therapeutic Intervention and Viable Alternative to Taxanes in CRPC. Mol Cancer Res. 2017 Jun;15(6):660-669. doi: 10.1158/1541-7786.MCR-17-0028. Epub 2017 Feb 16. PubMed PMID: 28209757.

Chemical Structure

204302 - Lerociclib | CAS 1628256-23-4 (free base)

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