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JH-VIII-157-02

🥰Excellent
Catalog No. T15612Cas No. 1639422-97-1

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.

JH-VIII-157-02

JH-VIII-157-02

🥰Excellent
Purity: 98.02%
Catalog No. T15612Cas No. 1639422-97-1
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 SizePriceAvailabilityQuantity
1 mg$118In Stock
5 mg$253In Stock
10 mg$376In Stock
25 mg$588In Stock
50 mg$793In Stock
100 mg$1,090In Stock
1 mL x 10 mM (in DMSO)$259In Stock
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Purity:98.02%
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight465.55
FormulaC28H27N5O2
Cas No.1639422-97-1
SmilesCCc1cc2C(=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 & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.1480 mL10.7400 mL21.4800 mL107.3998 mL
5 mM0.4296 mL2.1480 mL4.2960 mL21.4800 mL
10 mM0.2148 mL1.0740 mL2.1480 mL10.7400 mL
20 mM0.1074 mL0.5370 mL1.0740 mL5.3700 mL
50 mM0.0430 mL0.2148 mL0.4296 mL2.1480 mL

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