DEL-22379 / IBBTEC, Vichem - LARVOL DELTA

Inhibiting ERK dimerization ameliorates BRAF-driven anaplastic thyroid cancer. (PubMed, Cell Mol Life Sci) - "Our findings establish that BRAF- and RAS-mutant thyroid cells respond differentially to DEL-22379, which cannot be explained by the previously described mechanism of action of the inhibitor. Nonetheless, DEL-22379 demonstrated significant anti-tumor effects against BRAF-mutant cells in vivo with an apparent lack of toxicity, making it an interesting candidate for the development of combinatorial treatments. Our data underscore the differences elicited by the specific driver mutation for thyroid cancer onset and progression, which should be considered for experimental and clinical approaches."

Journal • Endocrine Cancer • Oncology • Solid Tumor • Thyroid Gland Anaplastic Carcinoma • Thyroid Gland Carcinoma • BRAF

Combined JAK2 and ERK1/2 kinase inhibition as a potent therapeutic approach in myeloproliferative neoplasms (SOHC 2020) - "Our data demonstrate that ERK kinase activation should be targeted to enhance the corrective potential in MPN and that dual inhibition of JAK2 and ERK1/2 increases therapeutic efficacy."

Preclinical

[VIRTUAL] Combined JAK2 and ERK1 / 2 kinase inhibition as a new therapeutic approach for myeloproliferative neoplasias (DGHO 2020) - " We assessed ERK inhibitors interfering with ATP binding (LTT462, MK8353) or ERK dimerization (DEL22379) as single agents and in combination with the JAK2 inhibitor ruxolitinib. Our data demonstrate that dual inhibition of JAK2 and ERK1/2 enhances the corrective potential in MPN indicating that ERK kinases should be targeted to increase therapeutic efficacy."

Fibrosis • Hematological Disorders • Immunology • Myeloproliferative Neoplasm • Oncology • Thrombocytopenia • Thrombocytosis • CD34 • DUSP6 • JAK2

[VIRTUAL] Combined JAK2 and ERK1 / 2 kinase inhibition as a new therapeutic approach for myeloproliferative neoplasias (DGHO 2020) - " We assessed ERK inhibitors interfering with ATP binding (LTT462, MK8353) or ERK dimerization (DEL22379) as single agents and in combination with the JAK2 inhibitor ruxolitinib. Our data demonstrate that dual inhibition of JAK2 and ERK1/2 enhances the corrective potential in MPN indicating that ERK kinases should be targeted to increase therapeutic efficacy."

Fibrosis • Hematological Disorders • Immunology • Myeloproliferative Neoplasm • Oncology • Thrombocytopenia • Thrombocytosis • CD34 • DUSP6 • JAK2

[VIRTUAL] Combined JAK2 and ERK1 / 2 kinase inhibition as a new therapeutic approach for myeloproliferative neoplasias (DGHO 2020) - " We assessed ERK inhibitors interfering with ATP binding (LTT462, MK8353) or ERK dimerization (DEL22379) as single agents and in combination with the JAK2 inhibitor ruxolitinib. Our data demonstrate that dual inhibition of JAK2 and ERK1/2 enhances the corrective potential in MPN indicating that ERK kinases should be targeted to increase therapeutic efficacy."

Fibrosis • Hematological Disorders • Immunology • Myeloproliferative Neoplasm • Oncology • Thrombocytopenia • Thrombocytosis • CD34 • DUSP6 • JAK2

[VIRTUAL] Combined JAK2 and ERK1 / 2 kinase inhibition as a new therapeutic approach for myeloproliferative neoplasias (DGHO 2020) - " We assessed ERK inhibitors interfering with ATP binding (LTT462, MK8353) or ERK dimerization (DEL22379) as single agents and in combination with the JAK2 inhibitor ruxolitinib. Our data demonstrate that dual inhibition of JAK2 and ERK1/2 enhances the corrective potential in MPN indicating that ERK kinases should be targeted to increase therapeutic efficacy."

Fibrosis • Hematological Disorders • Immunology • Myeloproliferative Neoplasm • Oncology • Thrombocytopenia • Thrombocytosis • CD34 • DUSP6 • JAK2