1858206-58-2
Chemical Structure
Edralbrutinib
Synonym(s): TG-1701
- CAS No.: 1858206-58-2
- Formula:C26H21F2N5O3
- Molecular Weight:489.47
IUPAC Name: (R)-4-amino-1-(1-(but-2-ynoyl)pyrrolidin-3-yl)-3-(4-(2,6-difluorophenoxy)phenyl)-1,6-dihydro-7H-pyrrolo[2,3-d]pyridazin-7-one
InChIKey: DNPOFZXZJJDQLB-MRXNPFEDSA-N
SMILES: O=C1C2=C(C(N)=NN1)C(C(C=C3)=CC=C3OC(C(F)=CC=C4)=C4F)=CN2[C@@](CC5)([H])CN5C(C#CC)=O
Biological Activity: Edralbrutinib (TG-1701) is a highly selective, orally available irreversible BTK inhibitor, with an EC50 of 6.70 nM and a Kd of 3 nM against human BTK. Edralbrutinib inhibits downstream signaling of the B cell receptor, induces dephosphorylation of Ikaros Ser442/445, promotes nuclear exclusion of Ikaros, attenuates Ikaros gene signatures, and exerts anti-tumor activity. Edralbrutinib can be used in research related to B-cell non-Hodgkin lymphoma, chronic lymphocytic leukemia, mantle cell lymphoma, follicular lymphoma, and diffuse large B-cell lymphoma[1][2].
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Edralbrutinib | 99.75% | Edralbrutinib (TG-1701) is a highly selective, orally available irreversible BTK inhibitor, with an EC50 of 6.70 nM and a Kd of 3 nM against human BTK. Edralbrutinib inhibits downstream signaling of the B cell receptor, induces dephosphorylation of Ikaros Ser442/445, promotes nuclear exclusion of Ikaros, attenuates Ikaros gene signatures, and exerts anti-tumor activity. Edralbrutinib can be used in research related to B-cell non-Hodgkin lymphoma, chronic lymphocytic leukemia, mantle cell lymphoma, follicular lymphoma, and diffuse large B-cell lymphoma. | ||||||||||||||||||||
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- [1]. Ribeiro ML, et al. Antitumor Activity of the Novel BTK Inhibitor TG-1701 Is Associated with Disruption of Ikaros Signaling in Patients with B-cell Non-Hodgkin Lymphoma. Clin Cancer Res. 2021;27(23):6591-6601. [Content Brief]
- [2]. Chan Yoon Cheah, et al. The Selective Bruton Tyrosine Kinase (BTK) Inhibitor TG-1701 As Monotherapy and in Combination with Ublituximab and Umbralisib (U2) in Patients with B-Cell Malignancies. Blood (2021) 138 (Supplement 1): 1549.
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