TrkA 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S2891 GW441756

GW441756是一种有效的,选择性的TrkA抑制剂,IC50为2 nM,对c-Raf1和CDK2几乎没有抑制活性。

Selective TrkA, IC50: 2 nM
S1107 Danusertib (PHA-739358)

Danusertib (PHA-739358)是一种Aurora kinase抑制剂,作用于Aurora A/B/C,无细胞试验中IC50为13 nM/79 nM/61 nM,适度有效作用于Abl,TrkA,c-RET和FGFR1,对Lck,VEGFR2/3,c-Kit,CDK2等作用效果稍弱。Phase 2。

Selective TrkA, IC50: 31 nM
S1460 SP600125

SP600125是一种广谱JNK抑制剂,作用于JNK1,JNK2和JNK3,无细胞试验中IC50分别为40 nM,40 nM和90 nM,比作用于MKK4选择性高10倍,比作用于MKK3, MKK6, PKB,和PKCα选择性高25倍,比作用于ERK2, p38, Chk1, EGFR等选择性高100倍。

Selective TrkA, IC50: 70 nM
S8636 Selitrectinib (LOXO-195)

Selitrectinib (LOXO-195, BAY 2731954) is an orally available, highly potent, and selective TRK kinase inhibitor with low nanomolar inhibitory activity against TRKA G595R, TRKC G623R, and TRKA G667C, IC50s ranging from 2.0 to 9.8 nmol/L. It is more than 1,000-fold selective for 98% of non-TRK kinases tested.

Pan WT TRKA, IC50: 0.6 nM
S8901 Taletrectinib (DS-6051b)

Taletrectinib (DS-6051b, AB-106) is a new-generation selective ROS1/NTRK inhibitor with ic50 of 0.207 nM,0.622 nM,2.28 nM and 0.980 nM for ROS1,NTRK1,NTRK2 and NTRK3,respectively.

Pan TrkA, IC50: 0.622 nM
S6412 Altiratinib

Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM.

Pan TrkA, IC50: 0.85 nM
S8788 CH7057288

CH7057288 is a potent and selective TRK inhibitor with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB, and TRKC respectively.

Pan TrkA, IC50: 1.1 nM
S9662 UNC2025

UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively.

Pan TrkA, IC50: 1.67 nM
S8573 Sitravatinib (MGCD516)

Sitravatinib (MGCD516)是一种新型的、靶向多种参与调节S180肉瘤细胞生长的RTKs的小分子抑制剂,包括c-Kit, PDGFRβ, PDGFRα, c-Met和Axl。

Pan TRKA (NTRK1), IC50: 5 nM
S8407 PF-06273340

PF-06273340是一种高度有效的、具有激酶选择性的、耐受良好的泛Trk抑制剂,对TrkA、TrkB、TrkC的IC50值分别为6 nM、4 nM、3 nM。

Pan TrkA, IC50: 6 nM
S1124 BMS-754807

BMS-754807是一种有效的IGF-1R/InsR可逆性抑制剂,在无细胞试验中IC50为1.8 nM/1.7 nM,对Met,Aurora A/B,TrkA/B和Ron作用稍弱,对Flt3, Lck,MK2,PKA,PKC等几乎没有抑制活性。Phase 2。

Pan TrkA, IC50: 7.4 nM
S7519 GNF-5837

GNF-5837是一种选择性的,口服生物有效的泛TRK抑制剂,作用于TrkA,TrkB的IC50值分别为8 nM,和12 nM。

Pan TrkA, IC50: 8 nM
S8348 BMS-935177

BMS-935177 is a potent, reversible Bruton's Tyrosine Kinase (BTK) inhibitor with an IC50 value of 2.8 nM and demonstrates good kinase selectivity. It is more potent against BTK than other kinase, including the other Tec family kinases (TEC, BMX, ITK, and TXK) over which the compound is between 5- and 67-fold selective.

Pan TrkA, IC50: 30 nM
S7998 Entrectinib (RXDX-101)

Entrectinib (RXDX-101)是一种口服生物可利用的泛-TrkA/B/CROS1ALK 抑制剂,IC50范围为 0.1~1.7 nM。Phase 2。

Pan
S8511 Belizatinib (TSR-011)

Belizatinib (TSR-011)是一种有效的ALK(IC50=0.7 nM)和tropomyosin receptor kinase (TRK) (IC50<3 nM)抑制剂。

Pan