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Purity: ≥98%
GW441756 (GW-441756) is a novel, potent and selective inhibitor of TrkA (Tropomyosin-related kinase A) with potential anticancer activity. It exhibits no or minimal activity against c-Raf1 and CDK2, and its IC50 for inhibiting TrkA is 2 nM. TrkA kinase activity is involved in numerous biological processes, such as proliferation, differentiation, and apoptosis, and it can influence downstream signaling. In the human muscle sarcoma cancer cell line HTB114, GW 441756 demonstrates strong anti-proliferative activity. Treatment with GW 441756 dose-dependently inhibited proliferation and triggered apoptosis. In Ewing sarcoma, Trk inhibition decreases cell proliferation and increases the effects of chemotherapy drugs.
| Targets |
TrkA (IC50 = 2 nM)
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
GW 441756 is a particular inhibitor of Tropomyosin-related kinase A (TrkA) with an IC50 value of 2 nM; it has minimal effect on CDK2 and c-Raf1. 2 nM is the IC50 value.
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| Cell Assay |
GW441756 specifically and in a dose-dependent manner inhibited TrkA-induced cell death; however, no effect was observed in uninduced cells. In the lack of a DNA damage inducer, K-252a and GW441756 significantly reduced TrkA's capacity to induce the production of γH2AX. Furthermore, K-252a suppressed it during doxorubicin treatment-induced DNA damage, but GW441756 did not.
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| Animal Protocol |
Wistar male rats
10 mg/kg i.p. |
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| References |
| Molecular Formula |
C17H13N3O
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| Molecular Weight |
275.3
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| Exact Mass |
275.311
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| Elemental Analysis |
C, 74.17; H, 4.76; N, 15.26; O, 5.81
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| CAS # |
504433-23-2
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| Appearance |
Solid powder
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| SMILES |
CN1C=C(C2=CC=CC=C21)/C=C\3/C4=C(C=CC=N4)NC3=O
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| InChi Key |
NXNQLECPAXXYTR-LCYFTJDESA-N
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| InChi Code |
InChI=1S/C17H13N3O/c1-20-10-11(12-5-2-3-7-15(12)20)9-13-16-14(19-17(13)21)6-4-8-18-16/h2-10H,1H3,(H,19,21)/b13-9-
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| Chemical Name |
(3Z)-3-[(1-methylindol-3-yl)methylidene]-1H-pyrrolo[3,2-b]pyridin-2-one
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.6324 mL | 18.1620 mL | 36.3240 mL | |
| 5 mM | 0.7265 mL | 3.6324 mL | 7.2648 mL | |
| 10 mM | 0.3632 mL | 1.8162 mL | 3.6324 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Inhibition of TrkA-induced cell death by its specific inhibitor GW441756. Exp Mol Med. 2008 Jun 30; 40(3): 276–285. |
TrkA overexpression induces γH2AX production and PARP cleavage. Exp Mol Med. 2008 Jun 30; 40(3): 276–285. |
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