MYX1715 is an inhibitor of N-Myristoyltransferase (NMT) with a KD value of 0.09 nM. MYX1715 inhibits the proliferation of LU0884 and LU2511 with IC50 values of 44 nM and 9 nM. MYX1715 exhibits antitumor efficacy against neuroblastoma and gastric cancer in mouse models. MYX1715 can be used as ADC toxin[1][2].
in vivo
MYX1715 (12.5 and 25 mg/kg, a single dose for 20 days) prevents tumour growth in a Th-MYCN GEMM model, in a DLBCL xenograft model and in a gastric cancer xenograft model[1].
Animal Model:
Th-MYCN GEMM mice model, DLBCL xenograft mice model and gastric cancer xenograft mice model[1]
Dosage:
12.5 and 25 mg/kg
Administration:
a single dose for 20 days
Result:
Inhibited tumour growth in mice bearing tumors.
References
[1] Zhang J, et al. Dysregulation of MYC-Family Proteins Sensitises Cancers to NMT Inhibition: Identification of NMTi Sensitivity and Mechanism[J]. Cancer Research, 2023, 83(7_Supplement): 4871-4871. [2] Carr R, et al. N-Myristoyltransferase (NMT) inhibitors are completely novel payloads for Antibody Drug Conjugates that deliver extensive tumor regression at well tolerated doses[J].
