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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 | Availability | Quantity |
---|---|---|---|
1 mg | $118 | In Stock | |
5 mg | $253 | In Stock | |
10 mg | $376 | In Stock | |
25 mg | $588 | In Stock | |
50 mg | $793 | In Stock | |
100 mg | $1,090 | In Stock | |
1 mL x 10 mM (in DMSO) | $259 | 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 (WT):2 nM, EML4-ALK (G1202R):2 nM, EML4-ALK (C1156Y):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. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 25 mg/mL (53.70 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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