Lerociclib

G1T38 ( Lerociclib) 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.


Cat. No.: EX-A3076	Purity: >98%

For research only, Do not use for Human!

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Synonyms	G1T38
CAS No.	1628256-23-4
Purity	>98%
Formula	C26H34N8O
Mol Weight	474.6012
Appearance	solid powder
Solubility	Soluble in DMSO
Shelf Life	>2 years if stored properly
Storage	Powder -20℃ 2 years; In solvent -20℃ 1 month;
Shipping	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.

Reference:	[1]. Bisi JE, et al.. 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 Jun 27;8(26):42343-42358. doi: 10.18632/oncotarget.16216. PubMed PMID: 28418845; PubMed Central PMCID: PMC5522071. [2]. Stice JP, et al. 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.
CoA	CoA of Lerociclib

Smiles:	O=C1NCC2(N3C1=CC4=CN=C(NC5=NC=C(N6CCN(C(C)C)CC6)C=C5)N=C43)CCCCC2


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