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JH-VIII-157-02

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.

Catalog No. T15612Cas No. 1639422-97-1

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Purity:98.02%

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COA HPLC HNMR

JH-VIII-157-02

Catalog No. T15612Cas No. 1639422-97-1

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Pack Size	Price	Availability
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

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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 (C1156Y):2 nM, EML4-ALK (G1202R):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 Weight	465.55
Formula	C₂₈H₂₇N₅O₂
Cas No.	1639422-97-1

Storage & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	2.1480 mL	10.7400 mL	21.4800 mL	107.3998 mL
5 mM	0.4296 mL	2.1480 mL	4.2960 mL	21.4800 mL
10 mM	0.2148 mL	1.0740 mL	2.1480 mL	10.7400 mL
20 mM	0.1074 mL	0.5370 mL	1.0740 mL	5.3700 mL
50 mM	0.0430 mL	0.2148 mL	0.4296 mL	2.1480 mL

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Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

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