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c-Myc inhibitor 9 2799717-96-5

c-Myc inhibitor 9 2799717-96-5

CAS No.: 2799717-96-5

c-Myc inhibitor 9 is a c-Myc inhibitor (antagonist) with logEC50 ≥6. c-Myc inhibitor 9 inhibits tumor growth in xenogra
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c-Myc inhibitor 9 is a c-Myc inhibitor (antagonist) with logEC50 ≥6. c-Myc inhibitor 9 inhibits tumor growth in xenograft nude mouse models. c-Myc inhibitor 9 may be utilized in cancer research.

Physicochemical Properties


Molecular Formula C27H31N5OS
Molecular Weight 473.63
Exact Mass 473.224
CAS # 2799717-96-5
PubChem CID 164572057
Appearance Typically exists as solid at room temperature
LogP 4.7
Hydrogen Bond Donor Count 2
Hydrogen Bond Acceptor Count 5
Rotatable Bond Count 7
Heavy Atom Count 34
Complexity 718
Defined Atom Stereocenter Count 0
InChi Key ACVCMFKUORPIPL-UHFFFAOYSA-N
InChi Code

InChI=1S/C27H31N5OS/c28-27(11-12-27)21-8-5-19(6-9-21)22-18-32-23-10-7-20(17-24(23)34-26(32)30-22)25(33)29-13-4-16-31-14-2-1-3-15-31/h5-10,17-18H,1-4,11-16,28H2,(H,29,33)
Chemical Name

2-[4-(1-aminocyclopropyl)phenyl]-N-(3-piperidin-1-ylpropyl)imidazo[2,1-b][1,3]benzothiazole-6-carboxamide
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)

Biological Activity


ln Vitro In A549 cells expressing c-Myc, c-Myc inhibitor 9 exhibits a logEC50 value of ≥6, indicating its effectiveness against Myc [1].
ln Vivo In A549 xenograft nude mice, c-Myc inhibitor 9 (3 mg/kg; intraperitoneal injection, twice a week, 49 days) efficiently inhibits tumor growth [1].
Animal Protocol Animal/Disease Models: NMRI female nude mice with A549 xenografts[1]
Doses: 3 mg/kg
Route of Administration: intraperitoneal (ip)injection; 3 mg/kg, twice a week, for 49 days
Experimental Results: diminished tumor volume.
References

[1]. Preparation of heteroaryl compounds as c-MYC mRNA translation modulators and uses thereof in the treatment of cancer. WO2022150316. 2022.


Solubility Data


Solubility (In Vitro) May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo) Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)

Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1114 mL 10.5568 mL 21.1135 mL
5 mM 0.4223 mL 2.1114 mL 4.2227 mL
10 mM 0.2111 mL 1.0557 mL 2.1114 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.