ALW-II-41-27

Alias: ALWII-41-27; ALW-II-41-27; ALW II-41-27; ALW II-4127; ALW-II-4127; ALWII-4127

Cat No.:V8240 Purity: ≥98%

COA Product Data Instructions for use SDS

ALW-II-41-27 is a potent Eph receptor tyrosine kinase inhibitor withIC50 of 11 nM for Eph2.

ALW-II-41-27 Chemical Structure CAS No.: 1186206-79-0
Product category: Ephrin Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Citations by Top Journals: Nature, Cell, Science, etc.

Top Publications Citing lnvivochem Products

Nature 2021, 597(7874):119-125.

Cell 2020,183:1202-1218.e25.

Science Adv 2022: 8, eabm9427.

Nature 597, 119–125 (2021)

Cell Stem Cell 2020,26(6):845-861.e12.

Science Trans Med 2023,15(701):eadd7872.

STTT 2023,8(1):91.

Cell Reports 2023,42(4):112313

Science Trans Med 2023, 15: eadd7872.

Cancer Cell 2021,39(4):529-547.e7.

Cancer Discov 2022,12(4):1106-1127.

Immunity 2023,56(3):620-634.e11.

J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

Biomaterial 2023 Sep16:302:122333.

Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Biological Data

Product Description

ALW-II-41-27 is a potent Eph receptor tyrosine kinase inhibitor with IC50 of 11 nM for Eph2. Tumor growth in vivo was inhibited by ALW-II-41-27'sinhibitionof EPHA2, which also reduced the survival and proliferation of erlotinib-resistant tumor cells. The viability of cells that had developed resistance to the third-generation EGFR TKI AZD9291 was likewise effectively decreased by ALW-II-41-27. All of these findings point to an involvement of EPHA2 in the preservation of cell survival in EGFR-mutant, TKI-resistant lung cancer and suggest that EPHA2 might be a valuable target for therapeutic intervention in these tumors.

Biological Activity I Assay Protocols (From Reference)

Targets	EphA2 (Kd = 12 nM)
ln Vitro	ALW-II-41-27 inhibits Ba/F3 cells transformed with Tel fusions of EphA3, Kit, Fms, KDR, FLT1, FGR, Src, Lyn, Bmx, and Bcr-Abl with an EC50 below 500 nM. Bcr-Abl and ALW-II-41-27 show cross-reactivity. Inhibiting b-raf, CSF1R, DDR1, DDR2, EphA2, EphA5, EphA8, EphB1, EphB2, EphB3, Frk, Kit, Lck, p38α, p38β, PDGFRα, PDGFRβ, Raf1, and numerous other kinases, ALW-II-41-27 shows how the addition of a thiophene group can significantly affect kinase selectivity[1].
Cell Assay	In order to ascertain the function of EPHA2, myogenic precursors were exposed to ALW-II-41-27 (0.5 μM) for a duration of 12 hours in GM, after which they underwent myogenic differentiation.
References	[1]. Discovery and structural analysis of Eph receptor tyrosine kinase inhibitors. Bioorganic & Medicinal Chemistry Letters (2009), 19(15), 4467-4470. [2]. Targeting EphA2 impairs cell cycle progression and growth of basal-like/triple-negative breast cancers. Oncogene. 2017 Jun 5.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula	C32H32F3N5O2S
Molecular Weight	607.6890
Exact Mass	607.22
Elemental Analysis	C, 63.25; H, 5.31; F, 9.38; N, 11.52; O, 5.27; S, 5.28
CAS #	1186206-79-0
Related CAS #	1186206-79-0
Appearance	Solid powder
SMILES	CCN1CCN(CC1)CC2=C(C=C(C=C2)NC(=O)C3=CC(=C(C=C3)C)NC(=O)C4=CN=CC(=C4)C5=CC=CS5)C(F)(F)F
InChi Key	HYWXBDQAYLPMIX-UHFFFAOYSA-N
InChi Code	InChI=1S/C32H32F3N5O2S/c1-3-39-10-12-40(13-11-39)20-23-8-9-26(17-27(23)32(33,34)35)37-30(41)22-7-6-21(2)28(16-22)38-31(42)25-15-24(18-36-19-25)29-5-4-14-43-29/h4-9,14-19H,3,10-13,20H2,1-2H3,(H,37,41)(H,38,42)
Chemical Name	N-[5-[[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]carbamoyl]-2-methylphenyl]-5-thiophen-2-ylpyridine-3-carboxamide
Synonyms	ALWII-41-27; ALW-II-41-27; ALW II-41-27; ALW II-4127; ALW-II-4127; ALWII-4127
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 Data

Solubility (In Vitro)	DMSO: ~100 mg/mL (~164.6 mM) Ethanol: ~100 mg/mL (~164.6 mM)

Preparing Stock Solutions		1 mg	5 mg	10 mg
	1 mM	1.6456 mL	8.2279 mL	16.4558 mL
	5 mM	0.3291 mL	1.6456 mL	3.2912 mL
	10 mM	0.1646 mL	0.8228 mL	1.6456 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.

Calculator

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

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The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

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The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)

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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.

Note： (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.

Biological Data

Pharmacologic inhibition of EphA2 recapitulates effects of genetic ablation. (a–c) MDA-MB-231 and wild-type (WT) C3-TAg tumor cells were grown in the presence of increasing concentrations of an EphA2 small molecule tyrosine kinase inhibitor ALW-II-41-27 (ALW) versus analog control and growth assessed by MTT assay after 72 h in culture. Oncogene . 2017 Oct 5;36(40):5620-5630.