Trk receptor
Signaling Pathway Map
Research Area
- Inhibitory Selectivity
- Solubility
| Catalog No. | Product Name | Solubility(25°C) | ||
|---|---|---|---|---|
| Water | DMSO | Alcohol | ||
| S1124 | BMS-754807 | <1 mg/mL | 92 mg/mL | 92 mg/mL |
| S2891 | GW441756 | <1 mg/mL | 25 mg/mL | <1 mg/mL |
| S7519 | GNF-5837 | <1 mg/mL | 100 mg/mL | 9 mg/mL |
| S8348 | BMS-935177 | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S7998 | Entrectinib (RXDX-101) | <1 mg/mL | 100 mg/mL | 75 mg/mL |
| S8573 | Sitravatinib (MGCD516) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S8407 | PF-06273340 | <1 mg/mL | 95 mg/mL | 1 mg/mL |
| S8511 | Belizatinib (TSR-011) | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S7960 | Larotrectinib (LOXO-101) sulfate | <1 mg/mL | 100 mg/mL | 100 mg/mL |
| S7745 | ANA-12 | <1 mg/mL | 37 mg/mL | <1 mg/mL |
| S8319 | 7,8-Dihydroxyflavone | <1 mg/mL | 50 mg/mL | 1 mg/mL |
Isoform-specific Inhibitors
Trk receptor Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1124 |
BMS-754807BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2. |
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| S2891 |
GW441756GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. |
Effect of TrkA inhibitorGW441756 on vorinostat andNGFmediated ERK phosphorylation. A)NS-1 cellswere treatedwith vorinostat (1 and 2.5 μM) andNGF (2.5 ng/mL)with and without GW441756 (1 μM) for 3 h. The blots were probed with anti-pERK.1/2 antibody. Vorinostat mediated activation of ERK1/2 phosphorylation (pErk) was abolished in presence of GW441756. Total ERK levels were checked using ERK 1/2 antibody. B) Bar graph represents the densitometric analysis of immunoblots. X axis represents treatments and Y axis represents the ratio of absolute relative density of pERK to the total ERK. The data sets are the mean ± SE of two biological replicates from two independent experiments (values compared to control vs vorinostat 1 μM and 2.5 μM, vorinostat 1 μM and 2.5 μM Vs GW441756 + vorinostat 1 and 2.5 μM respectively). *P < 0.05, **P < 0.001, ***P < 0.0001 indicate significant differences and ns indicates non-significant difference.
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|
| S7519 |
GNF-5837GNF-5837 is a selective, and orally bioavailable pan-TRK inhibitor for TrkA, and TrkB with IC50 of 8 nM, and 12 nM, respectively. |
||
| S8348New |
BMS-935177BMS-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. |
||
| S7998 |
Entrectinib (RXDX-101)Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2. |
Tumor cells were treated with entrectinib (10 nmol/L) for 4 hours or c-PARP for 48 hours, and harvested lysates were assessed by Western blotting. Data shown are representative of three independent experiments with similar results.
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| S8573 |
Sitravatinib (MGCD516)Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl. |
||
| S8407 |
PF-06273340PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively. |
||
| S8511 |
Belizatinib (TSR-011)"Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C). " |
||
| S7960 |
Larotrectinib (LOXO-101) sulfateLarotrectinib (LOXO-101) sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). |
Quantification of colony formation in (A), shown as a percentage of the control for NCIH2077 and RT112. Mean (3 biological replicates) +/- standard deviation (SD) shown (* p-value < 0.05, ** < 0.005, *** < 0.0005, two-sided t-test, comparing combination treatment to BGJ398 treatment). ns = not significant. (BGJ, BGJ398; Tram, Trametinib; BKM, BKM120; AZD, 8931; LDC, LDC1267; LOXO, LOXO-101; Imat, Imatinib; MGCD, MGCG-265).
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|
| S7745 |
ANA-12ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively. |
Maternal exercise ameliorated sevoflurane-induced neuronal cell loss and decreased dendritic spine density, blocked by TrkB inhibition. Nissl staining and Golgi staining were performed after behavior tests (n = 3). (A) Nissl staining in the CA1 region of hippocampus under ×400. (B) Neuronal density ratio changes. (C) Golgi staining in the CA1 of hippocampus under ×1000. (D) Histograms represented the number of dendritic spines/10 μm. Values are mean ± S.E.M. *p < 0.05, compared with Ctrl group; **p < 0.01, compared with Ctrl group; ##p < 0.01, compared with Sevo group; ∧∧p < 0.01, compared with Sevo + ME group. One-way analysis of variance followed by Tukey post hoc multiple comparison tests was used for data analysis.
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| S8319 |
7,8-Dihydroxyflavone7,8-Dihydroxyflavone acts as a potent and selective small-molecule agonist of the TrkB receptor (Kd ≈ 320 nM), the main signaling receptor of brain-derived neurotrophic factor (BDNF). |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1124 |
BMS-754807BMS-754807 is a potent and reversible inhibitor of IGF-1R/InsR with IC50 of 1.8 nM/1.7 nM in cell-free assays, less potent to Met, Aurora A/B, TrkA/B and Ron, and shows little activity to Flt3, Lck, MK2, PKA, PKC etc. Phase 2. |
|
|
| S2891 |
GW441756GW441756 is a potent, selective inhibitor of TrkA with IC50 of 2 nM, with very little activity to c-Raf1 and CDK2. |
Effect of TrkA inhibitorGW441756 on vorinostat andNGFmediated ERK phosphorylation. A)NS-1 cellswere treatedwith vorinostat (1 and 2.5 μM) andNGF (2.5 ng/mL)with and without GW441756 (1 μM) for 3 h. The blots were probed with anti-pERK.1/2 antibody. Vorinostat mediated activation of ERK1/2 phosphorylation (pErk) was abolished in presence of GW441756. Total ERK levels were checked using ERK 1/2 antibody. B) Bar graph represents the densitometric analysis of immunoblots. X axis represents treatments and Y axis represents the ratio of absolute relative density of pERK to the total ERK. The data sets are the mean ± SE of two biological replicates from two independent experiments (values compared to control vs vorinostat 1 μM and 2.5 μM, vorinostat 1 μM and 2.5 μM Vs GW441756 + vorinostat 1 and 2.5 μM respectively). *P < 0.05, **P < 0.001, ***P < 0.0001 indicate significant differences and ns indicates non-significant difference.
|
|
| S7519 |
GNF-5837GNF-5837 is a selective, and orally bioavailable pan-TRK inhibitor for TrkA, and TrkB with IC50 of 8 nM, and 12 nM, respectively. |
||
| S8348New |
BMS-935177BMS-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. |
||
| S7998 |
Entrectinib (RXDX-101)Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. Phase 2. |
Tumor cells were treated with entrectinib (10 nmol/L) for 4 hours or c-PARP for 48 hours, and harvested lysates were assessed by Western blotting. Data shown are representative of three independent experiments with similar results.
|
|
| S8573 |
Sitravatinib (MGCD516)Sitravatinib (MGCD516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl. |
||
| S8407 |
PF-06273340PF-06273340 is a highly potent, kinases elective, well-tolerated pan-Trk inhibitor with IC50 values of 6, 4, 3 nM for TrkA, TrkB, Trk C, respectively. |
||
| S8511 |
Belizatinib (TSR-011)"Belizatinib (TSR-011) is a potent inhibitor of ALK (IC50=0.7 nM) and tropomyosin receptor kinase (TRK) (IC50 values less than 3 nM for TRK A, B, and C). " |
||
| S7960 |
Larotrectinib (LOXO-101) sulfateLarotrectinib (LOXO-101) sulfate is an oral potent and selective ATP-competitive inhibitor of tropomyosin receptor kinases (TRK). |
Quantification of colony formation in (A), shown as a percentage of the control for NCIH2077 and RT112. Mean (3 biological replicates) +/- standard deviation (SD) shown (* p-value < 0.05, ** < 0.005, *** < 0.0005, two-sided t-test, comparing combination treatment to BGJ398 treatment). ns = not significant. (BGJ, BGJ398; Tram, Trametinib; BKM, BKM120; AZD, 8931; LDC, LDC1267; LOXO, LOXO-101; Imat, Imatinib; MGCD, MGCG-265).
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7745 |
ANA-12ANA-12 is a selective TrkB antagonist with Kd of 10 nM and 12 μM for the high and low affinity sites, respectively. |
2017, 2017:7984327 2018, 10.3389/fncel.2018.00122 2018, 10.1152/ajpheart.00245.2018 |
Maternal exercise ameliorated sevoflurane-induced neuronal cell loss and decreased dendritic spine density, blocked by TrkB inhibition. Nissl staining and Golgi staining were performed after behavior tests (n = 3). (A) Nissl staining in the CA1 region of hippocampus under ×400. (B) Neuronal density ratio changes. (C) Golgi staining in the CA1 of hippocampus under ×1000. (D) Histograms represented the number of dendritic spines/10 μm. Values are mean ± S.E.M. *p < 0.05, compared with Ctrl group; **p < 0.01, compared with Ctrl group; ##p < 0.01, compared with Sevo group; ∧∧p < 0.01, compared with Sevo + ME group. One-way analysis of variance followed by Tukey post hoc multiple comparison tests was used for data analysis.
|
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S8319 |
7,8-Dihydroxyflavone7,8-Dihydroxyflavone acts as a potent and selective small-molecule agonist of the TrkB receptor (Kd ≈ 320 nM), the main signaling receptor of brain-derived neurotrophic factor (BDNF). |
