Lerociclib(G1T38) - Moligand™, ≥99% , Inhibitor of cyclin dependent kinase 4;Inhibitor of cyclin dependent kinase 6, CAS No.1628256-23-4, Inhibitor of cyclin dependent kinase 4;Inhibitor of cyclin dependent kinase 6

CAS: 1628256-23-4 Cat. No.: G414063 Molecular Weight: 474.60

COA

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G1T38 - Moligand™, ≥99% CAS No(1628256-23-4) by Aladdin Scientific

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AVAILABLE TO ORDER

GRADE & PURITY Moligand™ ? ≥99%

Synonyms

G1T38; Lerociclib | 7',8'-Dihydro-2'-((5-(4-(1-methylethyl)-1-piperazinyl)-2-pyridinyl)amino)spiro(cyclohexane-1,9'(6'H)-pyrazino(1',2':1,5)pyrrolo(2,3-d)pyrimidin)-6'-one | HY-112272 | US9464092, GG | 2'-((5-(4-isopropylpiperazin-1-yl)pyridin-2-yl)amino)

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview Specifications Product Properties Names and Identifiers Documentation Advanced Data Taxonomic Classification 3D Structure Associated Targets(Human) Associated Targets(non-human) Mechanisms of Action Certificates（CoA,COO,BSE/TSE and Analysis Chart) Chemical and Physical Properties Solution Calculators Reviews

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Why this grade

Moligand™, ≥99% Moligand™ for sensitive chromatographic and analytical workflows requiring minimal baseline interference.

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Storage & shipping

Store at -20°C Ships Ice chest + Ice pads Check lot-specific COA for exact specifications.

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Quality documents

SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.

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Literature proof

Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.

Overview

Targets

CDK4 (Cell-free assay); CDK6 (Cell-free assay); CDK9 (Cell-free assay) 1 nM; 2 nM; 28 nM

In vitro

G1T38 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 vivo

G1T38 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

Specifications

Synonyms

G1T38; Lerociclib | 7', 8'-Dihydro-2'-((5-(4-(1-methylethyl)-1-piperazinyl)-2-pyridinyl)amino)spiro(cyclohexane-1, 9'(6'H)-pyrazino(1', 2':1, 5)pyrrolo(2, 3-d)pyrimidin)-6'-one | HY-112272 | US9464092, GG | 2'-((5-(4-isopropylpiperazin-1-yl)pyridin-2-yl)amino)

Specifications & Purity

Moligand™, ≥99%

Biochemical and Physiological Mechanisms

Lerociclib (G1T38) is a potent and selective inhibitor of CDK4/6, with IC50s of 1 nM, 2 nM for CDK4/CyclinD1 and CDK6/CyclinD3, respectively.

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Inhibitor of cyclin dependent kinase 4;Inhibitor of cyclin dependent kinase 6

Purity

≥99%

Product Properties

ALogP	4.087
hba_count	4
HBD Count	2
Rotatable Bond	4

Names and Identifiers

Canonical Smiles	CC(C)N1CCN(CC1)C2=CN=C(C=C2)NC3=NC=C4C=C5C(=O)NCC6(N5C4=N3)CCCCC6
IUPAC Name	4-[[5-(4-propan-2-ylpiperazin-1-yl)pyridin-2-yl]amino]spiro[1,3,5,11-tetrazatricyclo[7.4.0.02,7]trideca-2,4,6,8-tetraene-13,1'-cyclohexane]-10-one
InChIKey	YPJRHEKCFKOVRT-UHFFFAOYSA-N
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)
Isomeric SMILES	CC(C)N1CCN(CC1)C2=CN=C(C=C2)NC3=NC=C4C=C5C(=O)NCC6(N5C4=N3)CCCCC6
Molecular Weight	474.60
Reaxy-Rn	27461901
Reaxys-RN_link_address	https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=27461901&ln=

Documentation

📋 Safety Data Sheet (SDS)

Comprehensive hazard, handling, storage, and regulatory compliance document.

Download SDS →

✅ Certificate of Analysis (COA)

Lot-specific quality data. Enter your lot number to retrieve the exact COA.

Look up COA →

📊 Datasheet

Quick-reference summary of product specifications and applications.

View datasheet →

🔬 Specification Sheet

Full quality attributes and acceptance criteria for this grade.

View spec sheet →

Advanced Data

Taxonomic Classification

Taxonomy Tree

Kingdom Organic compounds
- Superclass Organoheterocyclic compounds
  - Class Diazinanes
    - Subclass Piperazines

Kingdom	Organic compounds
Superclass	Organoheterocyclic compounds
Class	Diazinanes
Subclass	Piperazines
Intermediate Tree Nodes	Not available
Direct Parent	Pyridinylpiperazines
Alternative Parents	N-arylpiperazines Pyrrolo[2,3-d]pyrimidines 2-heteroaryl carboxamides Dialkylarylamines N-alkylpiperazines Aminopyridines and derivatives Aminopyrimidines and derivatives Imidolactams Pyrroles Heteroaromatic compounds Trialkylamines Secondary carboxylic acid amides Amino acids and derivatives Lactams Azacyclic compounds Hydrocarbon derivatives Organic oxides Organooxygen compounds
Molecular Framework	Aromatic heteropolycyclic compounds
Substituents	Pyridinylpiperazine - N-arylpiperazine - Pyrrolo[2,3-d]pyrimidine - Pyrrolopyrimidine - 2-heteroaryl carboxamide - Dialkylarylamine - Tertiary aliphatic/aromatic amine - Aminopyridine - Aminopyrimidine - N-alkylpiperazine - Pyridine - Pyrimidine - Imidolactam - Heteroaromatic compound - Pyrrole - Amino acid or derivatives - Carboxamide group - Lactam - Tertiary aliphatic amine - Tertiary amine - Secondary carboxylic acid amide - Carboxylic acid derivative - Azacycle - Organooxygen compound - Organonitrogen compound - Organic nitrogen compound - Organic oxide - Hydrocarbon derivative - Organic oxygen compound - Amine - Aromatic heteropolycyclic compound
Description	This compound belongs to the class of organic compounds known as pyridinylpiperazines. These are compounds containing a pyridinylpiperazine skeleton, which consists of a pyridine linked (not fused) to a piperazine by a bond by a single bond that is not part of a ring.
External Descriptors	Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61. DOI: 10.1186/s13321-016-0174-y

3D Structure

Associated Targets(Human)

CDK4 Tclin Cyclin-dependent kinase 4 (1 Activities)

Discover Target: CDK4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK2 Tchem Cyclin-dependent kinase 2 (2 Activities)

Discover Target: CDK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

FLT3 Tclin Receptor-type tyrosine-protein kinase FLT3 (2 Activities)

Discover Target: FLT3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TTK Tchem Dual specificity protein kinase TTK (1 Activities)

Discover Target: TTK

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NEK10 Tchem Serine/threonine-protein kinase Nek10 (1 Activities)

Discover Target: NEK10

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK6 Tclin Cyclin-dependent kinase 6 (1 Activities)

Discover Target: CDK6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

ULK2 Tchem Serine/threonine-protein kinase ULK2 (1 Activities)

Discover Target: ULK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

NUAK2 Tchem NUAK family SNF1-like kinase 2 (1 Activities)

Discover Target: NUAK2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CDK6 Tclin Cyclin-dependent kinase 6 (1724 Activities)

Discover Target: CDK6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CDK9 Tchem Cyclin-dependent kinase 9 (2495 Activities)

Discover Target: CDK9

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CDK2 Tchem Cyclin-dependent kinase 2 (9050 Activities)

Discover Target: CDK2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

FLT3 Tclin Tyrosine-protein kinase receptor FLT3 (13481 Activities)

Discover Target: FLT3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

TTK Tchem Dual specificity protein kinase TTK (2978 Activities)

Discover Target: TTK

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ULK2 Tchem Serine/threonine-protein kinase ULK2 (652 Activities)

Discover Target: ULK2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

NUAK2 Tchem NUAK family SNF1-like kinase 2 (630 Activities)

Discover Target: NUAK2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CDK4 Tclin Cyclin-dependent kinase 4/cyclin D1 (2340 Activities)

Discover Target: CDK4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CCNE1 Tchem Cyclin-dependent kinase 2/cyclin E1 (1877 Activities)

Discover Target: CCNE1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CCND3 Tchem CDK6/cyclin D3 (897 Activities)

Discover Target: CCND3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

NEK10 Tchem Serine/threonine-protein kinase Nek10 (176 Activities)

Discover Target: NEK10

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Associated Targets(non-human)

Cdk4 Cyclin-dependent kinase 4 (3 Activities)

Discover Target: Cdk4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SARS-CoV-2 (38078 Activities)

Explore this target

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mechanisms of Action

Certificates（CoA,COO,BSE/TSE and Analysis Chart)

C of A & Other Certificates(BSE/TSE, COO):

Analytical Chart:

Chemical and Physical Properties

Solubility	Solubility (25°C) In vitro DMSO: 1 mg/mL (2.1 mM); Water: Insoluble; Ethanol: Insoluble;
DMSO(mg / mL) Max Solubility	2
DMSO(mM) Max Solubility	4.21407501053519
Water(mg / mL) Max Solubility	＜1
Molecular Weight	474.600 g/mol
XLogP3	3.400
Hydrogen Bond Donor Count	2
Hydrogen Bond Acceptor Count	7
Rotatable Bond Count	4
Exact Mass	474.286 Da
Monoisotopic Mass	474.286 Da
Topological Polar Surface Area	91.200 Å²
Heavy Atom Count	35
Formal Charge	0
Complexity	750.000
Isotope Atom Count	0
Defined Atom Stereocenter Count	0
Undefined Atom Stereocenter Count	0
Defined Bond Stereocenter Count	0
Undefined Bond Stereocenter Count	0
The total count of all stereochemical bonds	0
Covalently-Bonded Unit Count	1

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