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Product introduction
KX2-391 (Tirbanibulin) 是第一个临床Src抑制剂(拟肽类),靶向作用于Src的肽底物位点,在癌细胞系中GI50为9-60 nM。KX2-391 是一种高选择性的Src 激酶抑制剂,IC50值为20 nM 。 KX2-391 是一种非ATP 竞争性Src抑制剂。KX2-391是第一种靶向Src激酶底物结合位点的抑制剂。KX2-391 抑制Src 催化的FAK、Shc、paxillin转磷酸化以及Src 激酶自磷酸化。KX2-391 对PDGFR、EGFR、JAK1、JAK2 和Lck 没有影响,证明其为选择性抑制剂。KX2-391还是一种微管蛋白聚合抑制剂,通过与异二聚体微管蛋白上特定的位点结合而起抑制作用。在细胞实验中,KX2-391在NIH3T3/c-Src527F和SYF/c-Src527F 细胞中显示出生长抑制作用,GI50 值分别为23 nM 和39 nM 。 由于Src 是细胞增殖、存活、迁移和侵袭的调节因子,KX2-391 针对各种实体瘤和许多白血病肿瘤是有效的。已经证实KX2-391抑制原发性肿瘤生长并抑制肿瘤转移。
Chinese name
特班布林, 酪氨酸蛋白激酶 SRC 抑制剂
English name
Tirbanibulin
Chinese alias
-
English alias
BCP9000828 | Tirbanibulin (KX2-391) | 2-(5-(4-(2-morpholinoethoxy)phenyl)pyridin-2-yl)-N-benzylacetamide | WHO 10864 | Klisyri | STK802182 | TIRBANIBULIN [INN] | Z56968279 | NCGC00346644-01 | 4V9848RS5G | NCGC00346644-05 | T0781 | 2-Pyridineacetamide, 5-(
CAS number
897016-82-9
molecular formula
C26H29N3O3
molecular weight
431.53 g/mol
Exact mass
-
PSA
63.700 Ų
Logp
2.9
Technical Documents
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Research chemical 1ml

Research chemical 1ml; supplied for laboratory research, analysis, inspection, and scientific procurement use; specifications: 1ml.

item number:K408930-1ml
Product model:1ml
level: 1ml
Lead Time:-
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