2241039-81-4
2241039-81-4
Chemical Structure
Londamocitinib
Synonym(s): AZD4604; JAK1-IN-7
- CAS No.: 2241039-81-4
- Formula:C28H31F2N7O4S
- Molecular Weight:599.65
IUPAC Name: (R)-N-(3-(5-fluoro-2-((2-fluoro-3-(methylsulfonyl)phenyl)amino)pyrimidin-4-yl)-1H-indol-7-yl)-3-methoxy-2-(4-methylpiperazin-1-yl)propanamide
InChIKey: JNUZADQZHYFJGW-JOCHJYFZSA-N
SMILES: FC1=C(S(C)(=O)=O)C=CC=C1NC2=NC(C3=CNC4=C3C=CC=C4NC([C@@H](COC)N5CCN(C)CC5)=O)=C(F)C=N2
Biological Activity: Londamocitinib (AZD4604) is a potent and selective JAK1 inhibitor with IC50 at 0.54 nM. Londamocitinib has anti-inflammatory activity[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Londamocitinib | 99.79% | Londamocitinib (AZD4604) is a potent and selective JAK1 inhibitor with IC50 at 0.54 nM. Londamocitinib has anti-inflammatory activity. | ||||||||||||||||||||
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Golidocitinib (Standard) | Golidocitinib (Standard) (AZD4205 (Standard)) is the analytical standard of Golidocitinib (HY-107361). This product is intended for research and analytical applications. Golidocitinib (AZD4205) is a selective JAK1 inhibitor, with an IC50 of 73 nM, weakly inhibits JAK2 (IC50>14.7 μM), and shows little inhibition on JAK3 (IC50>30 μM). | |||||||||||||||||||||
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Almonertinib mesylate | 99.67% | Almonertinib (HS-10296) mesylate is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations. Almonertinib mesylate shows great inhibitory activity against T790M, T790M/L858R and T790M/Del19 (IC50: 0.37, 0.29 and 0.21 nM, respectively), and is less effective against wild type (3.39 nM). Almonertinib mesylate is used for the research of the non-small cell lung cancer. | ||||||||||||||||||||
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JAK1-IN-4 | 99.26% | JAK1-IN-4 is a potent and selective JAK1 inhibitor, with IC50s of 85 nM, 12.8 μM and >30 μM for JAK1, JAK2, and JAK3, respectively. JAK1-IN-4 inhibits STAT3 phosphorylation in NCI-H 1975 cells (IC50, 227 nM). | ||||||||||||||||||||
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AZ13705339 | 98.57% | AZ13705339 is a highly potent and selective PAK1 inhibitor with IC50s of 0.33 nM and 59 nM for PAK1 and pPAK1, respectively. AZ13705339 has binding affinities to PAK1 and PAK2, with Kds of 0.28 nM and 0.32 nM, respectively. AZ13705339 can be used in the research of cancers. | ||||||||||||||||||||
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Oritinib mesylate | Oritinib (SH-1028) mesylate is a selective, orally active, and pyrimidine-based irreversible inhibitor of EGFR with an IC50 of 18 nM. Oritinib (SH-1028) mesylate exhibits potent activity against EGFR sensitive and resistant (T790 M) mutations. Oritinib (SH-1028) mesylate significantly inhibits proliferation of tumor cells with EGFR sensitive and resistant mutation. | |||||||||||||||||||||
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EGFR-IN-69 | 99.58% | EGFR-IN-69 (compound 17g) is a potent EGFR inhibitor, with IC50 values of 4.3, 6.6 and 25.6 nM against EGFRL858R/T790M/C797S, EGFRL858R/T790M, and EGFR19del/T790M/C797S, respectively. EGFR-IN-69 can be used for non-small-cell-lung-cancer (NSCLC) research. | ||||||||||||||||||||
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ALK-IN-23 | ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALKWT, ALKL1196M and ALKG1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity. | |||||||||||||||||||||
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DCLK1-IN-2 | DCLK1-IN-2 (compound I-5) is a potent DCLK1 inhibitor with an IC50 of 171.3 nM. DCLK1-IN-2 shows remarkable antiproliferative effects on SW1990 cell lines (IC50 of 0.6 μM) and in vivo antitumor potency. | |||||||||||||||||||||
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HG-14-10-04 | 98.53% | HG-14-10-04 is a potent ALK and mutant EGFR inhibitor with IC50s of 20 nM, 15.6 nM, 22.6 nM and 124.5 nM for ALK, EGFRLR/TM, EGFR19del/TM/CS and EGFRLR/TM/CS, respectively. HG-14-10-04 can be used to research anticancer. | ||||||||||||||||||||
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Abemaciclib methanesulfonate (Standard) | 99.76% | Abemaciclib (methanesulfonate) (Standard) is the analytical standard of Abemaciclib (methanesulfonate). This product is intended for research and analytical applications. Abemaciclib methanesulfonate (LY2835219 methanesulfonate) is a selective CDK4/6 inhibitor with IC50s of 2 nM and 10 nM for CDK4 and CDK6, respectively. | ||||||||||||||||||||
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References
- [1]. NILSSON, Karl, Magnus, et al. Jak1 selective inhibitors. WO2018134213A1.
- [2]. Nilsson M, et al. Discovery of the Potent and Selective Inhaled Janus Kinase 1 Inhibitor AZD4604 and Its Preclinical Characterization. J Med Chem. 2023 Oct 12;66(19):13400-13415. [Content Brief]
- [3]. Nilsson M, et al. Characterization of Selective and Potent JAK1 Inhibitors Intended for the Inhaled Treatment of Asthma. Drug Des Devel Ther. 2022 Aug 31;16:2901-2917. [Content Brief]
