Lerociclib
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.
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Chemical Information
| Name | Lerociclib |
|---|---|
| Iupac Chemical Name | 2'-((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 |
| Synonyms | G1T38; G1T-38; G1T 38; G1-T38; G1 T-38; G1 T38; Lerociclib |
| Molecular Formula | C26H34N8O |
| Molecular Weight | 474.613 |
| Smile | CC(C)N(CC1)CCN1C(C=N2)=CC=C2NC3=NC=C4C(N(C5(CCCCC5)CNC6=O)C6=C4)=N3 |
| InChiKey | YPJRHEKCFKOVRT-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 Number | 1628256-23-4 (free base) |
| Related CAS | 2097938-59-3 (HCl) ; 1628256-23-4 (free base) |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Pale yellow solid |
|---|---|
| Purity | 98% |
| Storage | 0 - 4 C for short term (days to weeks), or -20 C for long term (months). |
| Solubility | Soluble in DMSO |
| Handling | Avoid inhalation, contact with eyes and skin. Avoid dust and aerosol formation. Use only in areas with appropriate exhaust ventilation. |
| Shipping Condition | Shipped 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 Code | 2933999701 |
| Targets | CDK4/6 inhibitor |
|---|---|
| Mechanism | Lerociclib (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
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