Limertinib
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MedKoo CAT#: 465747

CAS#: 1934259-00-3

Description: Limertinib, also known as ASK120067, is an EGFR inhibitor. ASK120067 displayed potent in vitro inhibitory efficacy against Bruton's tyrosine kinase protein and interleukin-2-inducible T cell kinase protein via covalent binding. In cell-based assays, ASK120067 dose-dependently suppressed Bruton's tyrosine kinase phosphorylation and exhibited anti-proliferation potency by inducing apoptosis in numerous B-lymphoma cells. Meanwhile, it caused growth arrest and induced the apoptosis of T-cell leukemia cells by attenuating interleukin-2-inducible T cell kinase activation. Oral administration of ASK120067 led to significant tumor regression in B-cell lymphoma and T-cell leukemia xenograft models by weakening Bruton's tyrosine kinase and interleukin-2-inducible T cell kinase signaling, respectively.

Chemical Structure

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Limertinib
CAS# 1934259-00-3
Instruction

Theoretical Analysis

MedKoo Cat#: 465747
Name: Limertinib
CAS#: 1934259-00-3
Chemical Formula: C29H32ClN7O2
Exact Mass: 545.23
Molecular Weight: 546.072
Elemental Analysis: C, 63.79; H, 5.91; Cl, 6.49; N, 17.96; O, 5.86

Price and Availability

Size Price Availability Quantity
5mg USD 450 2 Weeks
10mg USD 750 2 Weeks
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Synonym: ASK120067; ASK 120067; ASK-120067; limertinib,

IUPAC/Chemical Name: N-(5-((5-chloro-4-(naphthalen-2-ylamino)pyrimidin-2-yl)amino)-2-((2-(dimethylamino)ethyl)(methyl)amino)-4-methoxyphenyl)acrylamide

InChi Key: QHPVTCLSVVUPOF-UHFFFAOYSA-N

InChi Code: InChI=1S/C29H32ClN7O2/c1-6-27(38)33-23-16-24(26(39-5)17-25(23)37(4)14-13-36(2)3)34-29-31-18-22(30)28(35-29)32-21-12-11-19-9-7-8-10-20(19)15-21/h6-12,15-18H,1,13-14H2,2-5H3,(H,33,38)(H2,31,32,34,35)

SMILES Code: CN(CCN(C)C)C1=CC(OC)=C(NC2=NC=C(Cl)C(NC3=CC(C=CC=C4)=C4C=C3)=N2)C=C1NC(C=C)=O

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: To be determined

Shelf Life: >2 years if stored properly

Drug Formulation: To be determined

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

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 546.07 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: Cui X, Wang S, Gao H, Li B, Shi Y, Guo H, Song T, Zheng X. Development of an LC-MS/MS method for quantifying ASK120067, a novel mutant-selective inhibitor of the epidermal growth factor receptor (EGFR) as well as its main metabolite in human plasma and its application in a pharmacokinetic study. J Chromatogr B Analyt Technol Biomed Life Sci. 2021 Jan 1;1162:122488. doi: 10.1016/j.jchromb.2020.122488. Epub 2020 Dec 7. PMID: 33360679.

2: Zhang T, Qu R, Chan S, Lai M, Tong L, Feng F, Chen H, Song T, Song P, Bai G, Liu Y, Wang Y, Li Y, Su Y, Shen Y, Sun Y, Chen Y, Geng M, Ding K, Ding J, Xie H. Discovery of a novel third-generation EGFR inhibitor and identification of a potential combination strategy to overcome resistance. Mol Cancer. 2020 May 13;19(1):90. doi: 10.1186/s12943-020-01202-9. Erratum in: Mol Cancer. 2021 Aug 17;20(1):102. PMID: 32404161; PMCID: PMC7218543.