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1mg |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Deltarasin (also known as Deltarasin hydrochloride) is a novel, high affinity and potent small molecule inhibitor of KRAS-PDEδ protein-protein interaction with potential antineoplastic activity. It inhibits KRAS-PDEδ interaction with a Kd of 38 nM for binding to purified PDEδ. The KRAS oncogene product is considered a major target in anticancer drug discovery. 5 mM of deltarasin completely inhibited PDEδ-KRAS interaction and released the insolubilized mCitrine-RHEB/KRAS6Q to the endomembrane system. This showed that deltarasin interfered with the binding of KRAS to PDEδ in cells and thereby inhibited its solubilization
ln Vitro |
Deltarasin inhibits the interaction between RAS and PDEδ in liver cells, with a Kd of 41 nM. When deltarasin inhibits the PDEδ-KRAS interaction, human pancreatic ductal adenocarcinoma cells that rely on oncogenic KRAS proliferate less[1].
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ln Vivo |
In nude mice with subcutaneous human Panc-Tu-I tumor cell xenografts, deltarasin (10 mg/kg, ip) reduces dose-dependent tumor growth[1].
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Animal Protocol |
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References |
[1]. Zimmermann G, et al. Small molecule inhibition of the KRAS-PDEδ interaction impairs oncogenic KRAS signalling. Nature. 2013 May 30;497(7451):638-42.
[2]. Agalioti T, et al. Mutant KRAS promotes malignant pleural effusion formation. Nat Commun. 2017 May 16;8:15205. doi: 10.1038/ncomms15205 |
Molecular Formula |
C40H37N5O
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Molecular Weight |
603.75
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CAS # |
1440898-61-2
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SMILES |
C1(C2=CC=C(OC[C@@H](N3C4=CC=CC=C4N=C3C5=CC=CC=C5)C6CCNCC6)C=C2)=NC7=CC=CC=C7N1CC8=CC=CC=C8
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InChi Key |
NCIOVAYUMQEQEU-VKZSUDIWSA-N
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InChi Code |
InChI=1S/C40H37N5O.3ClH/c1-3-11-29(12-4-1)27-44-36-17-9-7-15-34(36)42-39(44)32-19-21-33(22-20-32)46-28-38(30-23-25-41-26-24-30)45-37-18-10-8-16-35(37)43-40(45)31-13-5-2-6-14-31;;;/h1-22,30,38,41H,23-28H2;3*1H/t38-;;;/m1.../s1
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Chemical Name |
2-[4-[(2S)-2-(2-phenyl-1H-benzimidazol-1-yl)-2-(4-piperidinyl)ethoxy]phenyl]-1-(phenylmethyl)-1H-benzimidazole, trihydrochloride
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Synonyms |
Deltarasin hydrochloride; Deltarasin HCl; Deltarasin;
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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) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.6563 mL | 8.2816 mL | 16.5631 mL | |
5 mM | 0.3313 mL | 1.6563 mL | 3.3126 mL | |
10 mM | 0.1656 mL | 0.8282 mL | 1.6563 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.