SJ11646 | LCK PROTAC | Probechem Biochemicals

Chemical Structure : SJ11646

加入收藏

SJ11646 (SJ 11646, SJ-11646)

货号: PC-22647Not For Human Use, Lab Use Only.

SJ11646 is a potent, dasatinib-based, cereblon-mediated LCK PROTAC degrader with DC50 of 0.00838 pM in in KOPT-K1 T-ALL cells, cytotoxic IC50 of 0.083pM.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

获取报价单

* 请选择数量再加入购物车

or Bulk Inquiry

大包装，大折扣！

E-mail: sales@probechem.com

Tech Support: tech@probechem.com

生物&药学活性

SJ11646 is a potent, dasatinib-based, cereblon-mediated LCK PROTAC degrader with DC50 of 0.00838 pM in in KOPT-K1 T-ALL cells, cytotoxic IC50 of 0.083pM.
SJ11646 induces a loss of LCK phosphorylation (pLCK) in KOPT-K1 T-ALL cells.
SJ11646 (100nM) induces a 92.6% LCK degradation and complete loss of pLCK within 3 hours.
SJ11646 shows superior cytotoxicity relative to dasatinib against a panel of T-ALL blasts collected from 10 patient-derived xenografts (PDX).
SJ11646 shows lower toxicity than dasatinib in both CD34+ cells (LC50 of 726.42 and 92.88nM, respectively), with similar results in peripheral blood mononuclear cells (LC50 of 13.84 and 2.81nM for, respectively).
SJ11646 is a potent and selective degrader of ABL and SRC family kinases, retaines dasatinib's targeting selectivity without inducing new interactions with other kinases.
SJ11646 exhibits cytotoxicity with an estimated LC50 of 0.0123 pM in B-ALL cell line SUP-B15 which harbors the BCR-ABL fusion gene.
SJ11646 induces prolonged suppression of LCK signaling in vitro and in vivo, has superior in vivo anti-leukemic efficacy compared to dasatinib.

物理化学性质&存储条件

分子量	746.28
分子式	C36H40ClN9O5S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Hu J, et al. Sci Transl Med. 2022 Aug 24;14(659):eabo5228.

SJ11646 (SJ 11646, SJ-11646)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

SJ11646 (SJ 11646, SJ-11646)

生物&药学活性

物理化学性质&存储条件

参考文献

Bulk Inquiry

* Indicates a Required FieldYour information is safe with us.

询单

Get Quotation Now

* Indicates a Required FieldYour information is safe with us.