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Trk Receptors

Inhibitory Selectivity
Catalog No.Inhibitor Name TrkATrkBTrkCTrk receptorOther
A11059BMS-754807
**
***
Insulin Receptor,IGF-1R,Met
A16238GW441756
****
A16259Sitravatinib (MGCD516)
***
*
DDR2,EPHA3,Axl
A13877ANA-12
*
A13730GNF-5837
**
*
**
A15801Entrectinib (RXDX-101)
ALK,ROS1
A10053Tyrphostin AG 879
*
Her2
A10715Danusertib (PHA-739358)
*
Aurora A, Abl, RET, FGFR1, Aurora C, Aurora B
A15494LM22A-4
*
A15974Larotrectinib (LOXO-101) sulfate
A161237,8-Dihydroxyflavone

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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Catalog No. Product Name Application Product Information
A13877 SALE

ANA-12

TrkB 抑制剂
ANA-12 is a TrkB receptor antagonist that demonstrates a 2-site mode of action, preventing activation by BDNF non-competitively.
A16239

LOXO-101 sulfate

TRK 抑制剂
LOXO-101 is a small molecule that was designed to block the ATP binding site of the TRK family of receptors, with 2 to 20 nM cellular potency against the TRKA, TRKB, and TRKC kinases.
A16238

GW 441756

TrkA 抑制剂
GW 441756 is a specific Tropomyosin-related kinase A (TrkA) inhibitor with an IC50 value of 2 nM; little activity to c-Raf1 and CDK2.
A16123

7,8-Dihydroxyflavone

TrkB 激动剂
7,8-Dihydroxyflavone, a selective tyrosine kinase receptor B (neurotrophic factor/tropomyosin-receptor-kinase B; TrkB) agonist, may be used to help identify and differentiate the physiological effects and cell signaling pathways mediated by TrkB activation, such as those involving neuroprotection, memory, vasorelaxation and hypertension.
A15974

LOXO-101 (ARRY-470, Larotrectinib)

TRK 抑制剂
LOXO-101 is an orally bioavailable, potent, ATP-competitive inhibitor of TRKA, TRKB, and TRKC.
A15801

Entrectinib

TRK, ROS1, ALK 抑制剂
Entrectinib, also known as RXDX-101 and NMS-E628, is an oral small molecule inhibitor of TrkA, TrkB and TrkC, as well as ROS1 and ALK, with high potency and selectivity.
A15494 SALE

LM22A-4

TrkB 激动剂
LM22A-4 is a potent tropomyosin-related kinase B (TrkB) agonist (IC50 = 47 nM).
A15345

TLQP 21

VGF-derived peptide
TLQP 21, VGF-derived peptide; spans residues 556-576 of the precursor sequence.
A13730 SALE

GNF 5837

TRK 抑制剂
GNF-5837 is a potent, selective, and orally bioavailable pan-TRK inhibitor that inhibited tumor growth in a mouse xenograft model derived from RIE cells expressing both TRKA and NGF.
A12666

AZ 23

TrkA 抑制剂
AZ 23 is a potent and selective tyrosine kinase Trk inhibitor with IC50 to 2 and 8 nM for TrkA and TrkB respectively
A10053 SALE

Tyrphostin AG 879

HER2 抑制剂
Tyrphostin AG 879 is an inhibitor of the tyrosine kinase activity of nerve growth factor (NGF) TrkA.
A11059 SALE

BMS-754807

IGF-1R 抑制剂
BMS-754807 is an efficacious, orally active growth factor 1 receptor/insulin receptor family-targeted kinase inhibitor that may act in combination with a wide array of established anticancer agents.
A10715 SALE

Danusertib (PHA-739358)

Aurora 抑制剂
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Phase 2
A16259

Sitravatinib

RTK 抑制剂
Sitravatinib is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth.

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