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JH-VIII-157-02 is an inhibitor of ALK and inhibits echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) with IC50s of 2 nM for EML4-ALK G1202R, EML4-ALKwt, EML4-ALK C1156Y, EML4-ALK F1174L, and EML4-ALK F1174L.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $118 | In Stock | In Stock | |
| 5 mg | $253 | In Stock | In Stock | |
| 10 mg | $376 | In Stock | In Stock | |
| 25 mg | $588 | In Stock | In Stock | |
| 50 mg | $793 | In Stock | In Stock | |
| 100 mg | $1,090 | In Stock | In Stock | |
| 1 mL x 10 mM (in DMSO) | $259 | In Stock | In Stock |
| Description | JH-VIII-157-02 is an inhibitor of ALK and inhibits echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) with IC50s of 2 nM for EML4-ALK G1202R, EML4-ALKwt, EML4-ALK C1156Y, EML4-ALK F1174L, and EML4-ALK F1174L. |
| Targets&IC50 | EML4-ALK (F1174L):2 nM, EML4-ALK (G1202R):2 nM, EML4-ALK (C1156Y):2 nM, EML4-ALK (WT):2 nM |
| In vitro | JH-VIII-157-02 potently inhibits EML4-ALKS1206Y, EML4-ALKG1269A, EML4-ALKL1196M, EML4-ALK1151Tins, and EML4-ALKL1152R with IC50s of 2, 3, 58, 107 and 196 nM, respectively. JH-VIII-157-02 has selectivity at other kinases, including IRAK1, CLK4, RET, RET V804L, RET V804M and IRAK 4 with IC50s of 14 nM, 14 nM, 3 nM, 13 nM, 12 nM, and 465 nM, respectively[1]. |
| In vivo | In mice, JH-VIII-157-02 (10 mg/kg) exhibits good oral bioavailability and penetrates the central nervous system[1]. |
| Molecular Weight | 465.55 |
| Formula | C28H27N5O2 |
| Cas No. | 1639422-97-1 |
| Smiles | CCc1cc2C(=O)c3c([nH]c4cc(ccc34)C#N)C(C)(C)c2cc1-c1cnn(CC(=O)N(C)C)c1 |
| Relative Density. | 1.28 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 25 mg/mL (53.7 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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