Lazertinib
Lazertinib
Lazertinib
FOB
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Product details
Essential details
Shipping:Express Delivery
Product Introduction
Melting point 149-155 ℃
Boiling point676.6 ± 65.0 ° C (Predicted)
Density   1.71
Storage conditions+2Cto+8C
Solubilityin DMSO, concentration 15mg/ml
Acidity coefficient (pKa)9.80 ± 0.12 (Predicted)
Appearance White solid
colorWhite to off white
SensitivityLightSensitive
JNJ-7706621 is a pan CDK inhibitor with the strongest inhibitory effect on CDK1/2, with an IC50 of 9nM/4nM. Its selectivity towards CDChemicalbookK1/2 is more than 6 times higher than that towards CDK3/4/6. It can also effectively inhibit Aurora A/B, but has no inhibitory activity on Plk1 and Wee1.
JNJ-7706621 is highly effective against CDK1 and 2, with IC50 values of 3-9nM. JNJ-7706621 also inhibits CDK3, 4, and 6, with IC50 values of 58-253nM. JNJ-7706621 inhibits Aurora-A and B, with IC50 values of 11 and 15nM, respectively. JNJ-7706621 also inhibits VEGF-R2, FGF-R2, and GSK3 β, with IC50 values of 154-254nM. JNJ-7706621 inhibits a group of human cancer cells, including HeLa, HCT-116, SChembookK-OV-3, PC3, DU145, A375, MDA-MB-231, MES-SA, and MES-SA/Dx5, with IC50 values of 112-514nM. The inhibitory effect of JNJ-7706621 on the growth of normal cell lines, including MRC-5, HASMC, HUVEC, and HMVEC, is several times lower, with an IC50 of 3.67-5.42 μ M. 0.5-3 μ MJNJ-7706621 acts on HeLa or U937 cells, causing cell arrest in G2-M phase, inducing nuclear replication, activating apoptosis, and reducing colony formation.
Treatment of mice carrying A375 malignant melanoma human tumor transplant model with JNJ-7706621 at 100 or 125 mg/kg resulted in tumor regression.
JNJ-7706621 is a novel and effective broad-spectrum CDK and Aurora kinase inhibitor.
JNJ-7706621 is a pan CDK inhibitor with the strongest inhibitory effect on CDK1/2, with an IC50 of 9nM/4nM in cell-free assays. Its selectivity towards CChemicalbookDK1/2 is more than 6 times higher than that towards CDK3/4/6. It can also effectively inhibit Aurora A/B, but has no inhibitory activity on Plk1 and Wee1.
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