| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
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)
|
|
|---|---|---|
| ln Vitro |
|
|
| ln Vivo |
|
|
| 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.
|
|
| 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.
|
|
| Animal Protocol |
Wistar male rats
10 mg/kg i.p. |
|
| References | ||
| Additional Infomation |
3-[(1-methyl-3-indolyl)methylidene]-1H-pyrrolo[3,2-b]pyridin-2-one is a member of indoles.
|
| Molecular Formula |
C17H13N3O
|
|
|---|---|---|
| Molecular Weight |
275.3
|
|
| Exact Mass |
275.105
|
|
| Elemental Analysis |
C, 74.17; H, 4.76; N, 15.26; O, 5.81
|
|
| CAS # |
504433-23-2
|
|
| Related CAS # |
|
|
| PubChem CID |
9943465
|
|
| Appearance |
Orange to red solid powder
|
|
| Density |
1.3±0.1 g/cm3
|
|
| Boiling Point |
568.0±50.0 °C at 760 mmHg
|
|
| Flash Point |
297.3±30.1 °C
|
|
| Vapour Pressure |
0.0±1.6 mmHg at 25°C
|
|
| Index of Refraction |
1.708
|
|
| LogP |
2.9
|
|
| Hydrogen Bond Donor Count |
1
|
|
| Hydrogen Bond Acceptor Count |
2
|
|
| Rotatable Bond Count |
1
|
|
| Heavy Atom Count |
21
|
|
| Complexity |
461
|
|
| Defined Atom Stereocenter Count |
0
|
|
| SMILES |
O=C1/C(/C2=C(C([H])=C([H])C([H])=N2)N1[H])=C(\[H])/C1=C([H])N(C([H])([H])[H])C2=C([H])C([H])=C([H])C([H])=C12
|
|
| InChi Key |
NXNQLECPAXXYTR-LCYFTJDESA-N
|
|
| 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-
|
|
| Chemical Name |
(3Z)-3-[(1-methylindol-3-yl)methylidene]-1H-pyrrolo[3,2-b]pyridin-2-one
|
|
| Synonyms |
|
|
| HS Tariff Code |
2934.99.9001
|
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
|
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
|
|||
|---|---|---|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| 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. |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
