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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
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.
| Targets |
EphA2 (Kd = 12 nM)
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|---|---|
| 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].
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| 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.
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| References |
| Molecular Formula |
C32H32F3N5O2S
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|---|---|
| Molecular Weight |
607.6890
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| Exact Mass |
607.223
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| Elemental Analysis |
C, 63.25; H, 5.31; F, 9.38; N, 11.52; O, 5.27; S, 5.28
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| CAS # |
1186206-79-0
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| Related CAS # |
1186206-79-0
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| PubChem CID |
42628503
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| Appearance |
White to light yellow solid powder
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| LogP |
7.423
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
43
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| Complexity |
933
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| Defined Atom Stereocenter Count |
0
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| SMILES |
S1C([H])=C([H])C([H])=C1C1C([H])=NC([H])=C(C=1[H])C(N([H])C1=C(C([H])([H])[H])C([H])=C([H])C(=C1[H])C(N([H])C1C([H])=C([H])C(=C(C(F)(F)F)C=1[H])C([H])([H])N1C([H])([H])C([H])([H])N(C([H])([H])C([H])([H])[H])C([H])([H])C1([H])[H])=O)=O
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| InChi Key |
HYWXBDQAYLPMIX-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
N-[5-[[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]carbamoyl]-2-methylphenyl]-5-thiophen-2-ylpyridine-3-carboxamide
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| Synonyms |
ALWII-41-27; ALW-II-41-27; ALW II-41-27; ALW II-4127; ALW-II-4127; ALWII-4127
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~164.6 mM)
Ethanol: ~100 mg/mL (~164.6 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.11 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.11 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| 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.
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.
(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.
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