| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| ln Vitro |
DGY-06-116 has an IC50 of 2.6 nM at 1 hour, which is an efficient inhibitor of Src activation [2]. In cell lines with SRC activation from non-small cell lung cancer (NSCLC) and triple-negative breast cancer (TNBC), DGY-06-116 (Compound 15a; 0.01-10 μM; 72) demonstrates strong anti-apoptotic effects [1]. In NSCLC cells, 15a (1 μM; 2 hours) significantly inhibits SRC binding and SRC signaling [1].
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|---|---|
| ln Vivo |
DGY-06-116 (Compound 15a; 5 mg/kg, paired with 3 i.p. injections every 12 hours) is able to suppress SRC over lengthy periods of time in C57B6 mice, presumably because to its capacity to covalently target [1]. 06-116 ip medication (5 mg) has a short half-life and high exposure (T1/2=1.29 h, AUC=12 746.25 min·ng/mL)/kg) B6 mice [1].
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| Cell Assay |
Cell proliferation assay [1]
Cell Types: H1975 (non-small cell lung cancer, NSCLC), HCC827 (NSCLC) and MDA-MB-231 (triple-negative breast cancer, TNBC) cell line Tested Concentrations: 0.01, 0.1, 1, ]. 10 μM Incubation Duration: 72 hrs (hours) Experimental Results: Strong growth inhibition of all three cell lines with GR50 values of 0.3, 0.5 and 0.3 μM for H1975, HCC827 and MDA-MB-231 respectively. Western Blot Analysis[1] Cell Types: H1975 and HCC827 NSCLC Cell Tested Concentrations: 1 μM Incubation Duration: 2 hrs (hours) Experimental Results: p-SRCY416 signaling was inhibited in H1975 and HCC827 cells. |
| Animal Protocol |
Animal/Disease Models: Adult C57B6 mice[1]
Doses: 5 mg/kg Route of Administration: intraperitoneal (ip) injection; 3 times every 12 hrs (hrs (hours)) Experimental Results: Compared with vehicle control, induced p-SRCY416 at 2 hrs (hrs (hours)) and 4 hrs (hrs (hours)) after administration inhibition. SRC binding and inhibition were demonstrated at both 2 and 4 hrs (hrs (hours)) post-dose compared to vehicle control. |
| References |
| Molecular Formula |
C32H33CLN8O2
|
|---|---|
| Molecular Weight |
597.109824895859
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| Exact Mass |
596.241
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| CAS # |
2556836-50-9
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| PubChem CID |
154573782
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| Appearance |
White to off-white solid powder
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| LogP |
6
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
43
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| Complexity |
925
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1=CC=CC(C)=C1NC(C1C=NC(=NC=1NC1C=CC=CC=1NC(C=C)=O)NC1C=CC(=CC=1)N1CCN(C)CC1)=O
|
| InChi Key |
HLRQYOGLZWIOPA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H33ClN8O2/c1-4-28(42)36-26-10-5-6-11-27(26)37-30-24(31(43)38-29-21(2)8-7-9-25(29)33)20-34-32(39-30)35-22-12-14-23(15-13-22)41-18-16-40(3)17-19-41/h4-15,20H,1,16-19H2,2-3H3,(H,36,42)(H,38,43)(H2,34,35,37,39)
|
| Chemical Name |
N-(2-chloro-6-methylphenyl)-2-[4-(4-methylpiperazin-1-yl)anilino]-4-[2-(prop-2-enoylamino)anilino]pyrimidine-5-carboxamide
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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 : ~250 mg/mL (~418.68 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.48 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 20.8 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: ≥ 2.08 mg/mL (3.48 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6747 mL | 8.3737 mL | 16.7473 mL | |
| 5 mM | 0.3349 mL | 1.6747 mL | 3.3495 mL | |
| 10 mM | 0.1675 mL | 0.8374 mL | 1.6747 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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