Mycro3

Alias: Mycro3; Mycro-3; Mycro 3
Cat No.:V22075 Purity: ≥98%
Mycro 3 is an orally bioactive, potent and specific inhibitor of Myc-Max dimerization.
Mycro3 Chemical Structure CAS No.: 944547-46-0
Product category: c-Myc
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description
Mycro 3 is an orally bioactive, potent and specific inhibitor of Myc-Max dimerization. Mycro 3 could be used in pancreatic cancer research.
Biological Activity I Assay Protocols (From Reference)
Targets
AP-1; c-Myc
ln Vitro
In whole-cell experiments, Mycro 3 is a strong and sensitive c-Myc dye that exhibits a mild inhibitory effect against activator protein 1 (AP-1). The dye-reactive properties of Mycro 3 are identical to those of its predecessor. Mycro 3 prevents Myc and Max from coordinating with the c-Myc dye. Mycro 3 is a highly specific inhibitor of DNA binding and c-Myc/Max dimerization [1]. With IC50s of 0.25 and 9.0 μM for cells with intact Myc alleles and Myc-null cells, respectively, Mycro 3 shows excellent promise [2].
ln Vivo
In patients with pancreatic ductal adenocarcinoma (PDA), Mycro 3 (100 mg/kg; oral; taken daily for two months) significantly reduces cell swelling, enlarges the pancreas, and causes considerable shrinking. Significant differences were also observed in the growth of Mycro 3-treated NOD/SCID tumors containing orthotopic or heterotopic human pancreatic xenografts [2].
Animal Protocol
Animal/Disease Models: Moribund Pdx1-cre/KRAS* mice with pancreatic ductal adenocarcinoma (PDA) [2]
Doses: 100 mg/kg
Route of Administration: Oral; one time/day for two months
Experimental Results: Prolonged survival . Mycro 3 administration was stopped after two months, and the mice survived for another month.
References
[1]. Chen BJ, et al. Small molecules targeting c-Myc oncogene: promising anti-cancer therapeutics. Int J Biol Sci. 2014 Sep 13;10(10):1084-96.
[2]. Dimitris Stellas, et al. Therapeutic effects of an anti-Myc drug on mouse pancreatic cancer. J Natl Cancer Inst. 2014 Oct 11;106(12):dju320.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H17CLF2N6O4
Molecular Weight
526.88
Exact Mass
526.0968
Elemental Analysis
C, 54.71; H, 3.25; Cl, 6.73; F, 7.21; N, 15.95; O, 12.15
CAS #
944547-46-0
Related CAS #
944547-46-0
Appearance
Solid powder
SMILES
CCOC(=O)C1=C(N(N=C1)C2=CC=CC=C2)NC(=O)C3=NN4C(=CC(=NC4=C3)C5=CC=CO5)C(F)(F)Cl
InChi Key
YPPNLSKYXDXQGD-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H17ClF2N6O4/c1-2-36-23(35)15-13-28-32(14-7-4-3-5-8-14)21(15)30-22(34)17-12-20-29-16(18-9-6-10-37-18)11-19(24(25,26)27)33(20)31-17/h3-13H,2H2,1H3,(H,30,34)
Chemical Name
ethyl 5-[[7-[chloro(difluoro)methyl]-5-(furan-2-yl)pyrazolo[1,5-a]pyrimidine-2-carbonyl]amino]-1-phenylpyrazole-4-carboxylate
Synonyms
Mycro3; Mycro-3; Mycro 3
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 (~189.8 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 2.5 mg/mL (4.74 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
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 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 1.8980 mL 9.4898 mL 18.9797 mL
5 mM 0.3796 mL 1.8980 mL 3.7959 mL
10 mM 0.1898 mL 0.9490 mL 1.8980 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.

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

(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
  • Treatment of mouse pancreatic ductal adenocarcinoma (PDA) with Mycro3 administration. J Natl Cancer Inst . 2014 Oct 11;106(12):dju320.
  • Mycro3-treatment of xenografts generated by orthotopic or heterotopic transplantation of the human pancreatic ductal adenocarcinoma (PDA) cell lines Panc1 and MiaPaCa2. J Natl Cancer Inst . 2014 Oct 11;106(12):dju320.
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