SML3944
SJ11646
≥98% (HPLC)
别名:
N-(2-Chloro-6-methylphenyl)-2-((6-(4-(3-(2-(4-(2,6-dioxopiperidin-3-yl)phenoxy)acetamido)propyl)piperazin-1-yl)-2-methylpyrimidin-4-yl)amino)thiazole-5-carboxamide, SJ 1011646, SJ 11646, SJ-1011646, SJ-11646, SJ1011646
InChI key
AJNQGWOQPRWRML-UHFFFAOYSA-N
SMILES string
CC1=NC(NC2=NC=C(C(NC3=C(C=CC=C3Cl)C)=O)S2)=CC(N4CCN(CC4)CCCNC(COC5=CC=C(C=C5)C6CCC(NC6=O)=O)=O)=N1
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
-10 to -25°C
Quality Level
Biochem/physiol Actions
Potent ABL and SRC family tyrosine kinases (TYKs) degrader with greater antileukemic efficacy than dasatinib in cultures and in vivo.
SJ11646 is a potent and high-affinity (LCK/ABL1/SRC Kd = 0.14/0.054/0.17 nM for SJ11646 vs. 0.09/0.054/0.19 nM for dasatinib) ABL and SRC family tyrosine kinases (TYKs) degrader composed of dasatinib linked to a E3 ligase cereblon (CRBN)-binding ligand. SJ11646 effectively degrades SRC family TYKs in KOPT-K1 cells (LCK, CSK, SRC, FYN; 100 nM for 24h) and is 55,114-times more cytotoxic (LC50 = 0.0123 pM) than dasatinib against the BCR-ABL fusion-harboring B-ALL cell line SUP-B15. When used at equal molar amount via daily i.p., SJ11646 (15 mg/kg) shows significantly greater antileukemic efficacy than dasatinib (10 mg/kg) in two T-ALL PDX models in mice in vivo.
SJ11646 is a potent and high-affinity (LCK/ABL1/SRC Kd = 0.14/0.054/0.17 nM for SJ11646 vs. 0.09/0.054/0.19 nM for dasatinib) ABL and SRC family tyrosine kinases (TYKs) degrader composed of dasatinib linked to a E3 ligase cereblon (CRBN)-binding ligand. SJ11646 effectively degrades SRC family TYKs in KOPT-K1 cells (LCK, CSK, SRC, FYN; 100 nM for 24h) and is 55,114-times more cytotoxic (LC50 = 0.0123 pM) than dasatinib against the BCR-ABL fusion-harboring B-ALL cell line SUP-B15. When used at equal molar amount via daily i.p., SJ11646 (15 mg/kg) shows significantly greater antileukemic efficacy than dasatinib (10 mg/kg) in two T-ALL PDX models in mice in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Jianzhong Hu et al.
Science translational medicine, 14(659), eabo5228-eabo5228 (2022-08-25)
T cell acute lymphoblastic leukemia (T-ALL) is an aggressive hematological malignancy, and there is an unmet need for targeted therapies, especially for patients with relapsed disease. We have recently identified pre-T cell receptor and lymphocyte-specific protein tyrosine kinase (LCK) signaling
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