Lerociclib
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MedKoo CAT#: 206842

CAS#: 1628256-23-4 (free base)

Description: 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 (<100 nM) in Rb competent cell lines compared to >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.


Price and Availability

Size
Price

25mg
USD 350
200mg
USD 1650
2g
USD 5850
Size
Price

50mg
USD 650
500mg
USD 2650
Size
Price

100mg
USD 1050
1g
USD 3450

Lerociclib, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 206842
Name: Lerociclib
CAS#: 1628256-23-4 (free base)
Chemical Formula: C26H34N8O
Exact Mass: 474.2856
Molecular Weight: 474.613
Elemental Analysis: C, 65.80; H, 7.22; N, 23.61; O, 3.37


Related CAS #: 2097938-59-3 (HCl)   1628256-23-4 (free base)    

Synonym: G1T38; G1T-38; G1T 38; G1-T38; G1 T-38; G1 T38; 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

InChi Key: YPJRHEKCFKOVRT-UHFFFAOYSA-N

InChi Code: 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)

SMILES Code: CC(C)N(CC1)CCN1C(C=N2)=CC=C2NC3=NC=C4C(N(C5(CCCCC5)CNC6=O)C6=C4)=N3


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

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.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:
2934990300


Additional Information

Inhibition of the p16INK4a/cyclin D/CDK4/6/RB pathway is an effective therapeutic strategy for the treatment of estrogen receptor positive (ER+) breast cancer.


References

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 of
cyclin 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.