YH 25448
N-{5-[(4-{4-[(dimethylamino)methyl]-3-phenyl-1H-pyrazol-1-yl}pyrimidin-2-yl)amino]-4-methoxy-2-(morpholin-4-yl)phenyl}prop-2-enamide
CAS: 1903008-80-9
Molecular Formula: C30H34N8O3
YH 25448 - Names and Identifiers
YH 25448 - Physico-chemical Properties
| Molecular Formula | C30H34N8O3 |
| Molar Mass | 554.64 |
| Density | 1.27±0.1 g/cm3(Predicted) |
| Solubility | Soluble in DMSO |
| pKa | 12.39±0.70(Predicted) |
| Storage Condition | -20℃ |
| Use | Lazertinib, also known as YH-25448 and GNS-1480, is an oral active, highly potent, mutant-selective and irreversible EGFR Tyrosine-kinase inhibitors (TKIs) targets both the T790M mutation and activating EGFR mutations while sparing wild type-EGFR. YH25448 is expected to beneficial for the NSCLC patients with brain metastasis due to good blood brain barrier (BBB) penetration property as well as for the treatment of primary lung lesion and extracranial lesions. This study will be conducted to evaluate the safety, tolerability and efficacy of YH25448 in locally advanced or metastatic NSCLC patients with EGFR mutations. |
| In vitro study | Lazertinib was able to target EGFR activating mutants Del19, L858R and T790M, with a relatively small effect on wild-type EGFR. In NSCLC cell lines and in primary tumor cells (derived from patients with EGFR mutations), YH25448 inhibited the growth of cancer cells more effectively than osimertinib and significantly increased apoptosis of tumor cells. In the cell proliferation assay, the GI50 values of lazertinib for H1975 cells (L858R/T790M), PC9 cells (del19) and H2073 cells (wild-type EGFR) were 5 nM, 5 nM and 711 nM. |
| In vivo study | In vivo, YH25448 can cause non-significant, concentration-dependent tumor regression in subcutaneous and intracranial lesions when administered once daily to a mouse model transplanted with H1975 cells, without other abnormalities such as skin keratinization. The half-life of YH25448 in plasma is 5.9-6.8 hours, and the AUC 0-last ratio in tumor and plasma is 3.0-5.1. YH25448 can well cross the blood-brain barrier, and the concentration of cerebrospinal fluid can exceed the IC50 value of pEGFR inhibition. YH25448 also had good efficacy on tumor regression in a brain metastasis model with EGFR mutants. |
YH 25448 - Reference
| Reference Show more | 1. Byoung Chul Cho, et al. YH25448, a 3rd Generation EGFR-TKI, in Patients with EGFR-TKI-resistant NSCLC: Phase I/II Study Results. |
YH 25448 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.803 ml | 9.015 ml | 18.03 ml |
| 5 mM | 0.361 ml | 1.803 ml | 3.606 ml |
| 10 mM | 0.18 ml | 0.901 ml | 1.803 ml |
| 5 mM | 0.036 ml | 0.18 ml | 0.361 ml |
Last Update：2024-01-02 23:10:35
YH 25448 - Animal Experiment
Animal Models: An intracranial tumor growth model (BALB/c nude mice inoculate with H1975-luc cells)Dosages: 10 and 25 mg/kgAdministration: --
Last Update：2023-08-16 21:32:38
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Product Name: N-{5-[(4-{4-[(dimethylamino)methyl]-3-phenyl-1H-pyrazol-1-yl}pyrimidin-2-yl)amino]-4-methoxy-2-(morpholin-4-yl)phenyl}prop-2-enamide Visit Supplier Webpage Request for quotationCAS: 1903008-80-9
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QQ: 3008007409
Featured ProductsSpot supply
Product Name: Lazertinib (YH25448,GNS-1480) Visit Supplier Webpage Request for quotationCAS: 1903008-80-9
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328
WhatsApp: +86-18821248368
Spot supply
Product Name: Lazertinib Request for quotationCAS: 1903008-80-9
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365
Wechat: 18916960931
Spot supply
Product Name: Lazertinib Visit Supplier Webpage Request for quotationCAS: 1903008-80-9
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922
Wechat: 18621343501
WhatsApp: +86-18621343501
Spot supply
Product Name: YH25448; GNS-1480 Visit Supplier Webpage Request for quotationCAS: 1903008-80-9
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
Mobile: 609-228-6898
Spot supply
Product Name: N-{5-[(4-{4-[(dimethylamino)methyl]-3-phenyl-1H-pyrazol-1-yl}pyrimidin-2-yl)amino]-4-methoxy-2-(morpholin-4-yl)phenyl}prop-2-enamide Visit Supplier Webpage Request for quotationCAS: 1903008-80-9
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Mobile: 18021002903
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View History
YH 25448
4-nitrophenetole
普氧
101-89-3
Aluminiumfluoride1
ISOPROPYLAMINE DODECYLBENZENESULFONATE
30315-46-9
1032229-33-6
161735-79-1
37859-24-8
4-nitrophenetole
普氧
101-89-3
Aluminiumfluoride1
ISOPROPYLAMINE DODECYLBENZENESULFONATE
30315-46-9
1032229-33-6
161735-79-1
37859-24-8