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Purity: ≥98%
XMD16-5 is a novel and potent tyrosine kinase nonreceptor 2(TNK2) inhibitor with IC50s of 16 nmol/L and 77 nmol/L for the D163E and R806Q mutations. TNK2 mutations were found in renal cancer cells and also in lung, ovarian and gastric cancers. TNK2 genomic amplification has been associated with late stage or metastatic lung and prostate cancers. Overexpression of TNK2 promoted metastasis in a mouse model of breast cancer. TNK2 signaling is disrupted in prostate, breast and gastrointestinal tumors. XMD8-87 and XMD16-5 potently inhibit phosphorylation of TNK2 truncation mutations found in solid tumor types. XMD16-5 was identified from kinase inhibitor screens to predict functional gene targets in primary specimens from patients with acute myeloid leukemia and chronic myelomonocytic leukemia. Deep sequencing of the same patient specimens identified genetic alterations that were then integrated with the functionally important targets using the HitWalker algorithm to prioritize the mutant genes that most likely explain the observed drug sensitivity patterns.
| ln Vitro |
Even at the highest measured dosages (1,000 nM), XMD16-5 had little to no effect on control cells while potently inhibiting the proliferation of TNK2 mutant expressing cell lines. For the D163E and R806Q mutations, XMD16-5's IC50s are 16 nM and 77 nM, respectively. On-target effects on TNK2 account for the majority of XMD16-5's effects on TNK2 cell lines. With TNK2 inhibitor XMD16-5, auto-phosphorylation of overexpressed TNK2 mutants could be prevented[1].
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| References |
[1]. Maxson JE, et al. Identification and Characterization of Tyrosine Kinase Nonreceptor 2 Mutations in Leukemia through Integration of Kinase Inhibitor Screening and Genomic Analysis
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| Molecular Formula |
C23H24N6O2
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| Molecular Weight |
416.48
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| Exact Mass |
416.2
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| Elemental Analysis |
C, 66.33; H, 5.81; N, 20.18; O, 7.68
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| CAS # |
1345098-78-3
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| Appearance |
Solid powder
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| SMILES |
OC(CC1)CCN1C(C=C2)=CC=C2NC3=NC=C4C(N(C)C(C=CC=C5)=C5C(N4)=O)=N3
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.00 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 (6.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4011 mL | 12.0054 mL | 24.0108 mL | |
| 5 mM | 0.4802 mL | 2.4011 mL | 4.8022 mL | |
| 10 mM | 0.2401 mL | 1.2005 mL | 2.4011 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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