Deltarasin hydrochloride

Name: Deltarasin hydrochloride
Brand: MedChemExpress
SKU: HY-15747A
Rating: 4.5 (2 reviews)

Cat. No.: HY-15747A: FAQs
Data Sheet SDS COA Handling Instructions

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Deltarasin hydrochloride is an inhibitor of KRAS-PDEδinteraction with K_d of 38 nM for binding to purified PDEδ.

For research use only. We do not sell to patients.

Deltarasin hydrochloride Chemical Structure

CAS No. : 1613404-76-4

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 254	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 254	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 252	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 1008	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1800	Get quote	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Deltarasin hydrochloride:

Deltarasin In-stock
Deltarasin trihydrochloride Get quote

2 Publications Citing Use of MCE Deltarasin hydrochloride

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•Related Small Molecules:

•Related Proteins:

View All Ras Isoform Specific Products:

View All Isoforms

K-Ras H-Ras Ras

View All Phosphodiesterase (PDE) Isoform Specific Products:

View All Isoforms

PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Deltarasin hydrochloride is an inhibitor of KRAS-PDEδinteraction with K_d of 38 nM for binding to purified PDEδ.

IC₅₀ & Target

Kd: 38 nM (PDEδ)

In Vitro

In liver cells, deltarasin inhibits the interaction of RAS with PDEδ with K_D of 41 nM. Inhibition of PDEδ-KRAS interaction by deltarasin suppresses proliferation of human pancreatic ductal adenocarcinoma cells that are dependent on oncogenic KRAS^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Deltarasin (10 mg/kg, i.p.) impairs dose-dependent tumor growth in nude mice bearing subcutaneous human Panc-Tu-I tumour cell xenografts^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

640.22

Formula

C₄₀H₃₈ClN₅O

CAS No.

1613404-76-4

Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility

In Vitro:

DMSO : ≥ 52 mg/mL (81.22 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 50 mg/mL (78.10 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.5620 mL	7.8098 mL	15.6196 mL
5 mM	0.3124 mL	1.5620 mL	3.1239 mL
10 mM	0.1562 mL	0.7810 mL	1.5620 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 98.07%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (256 KB) LCMS (95 KB)

Handling Instructions (2659 KB)

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. [Content Brief]

Kinase Assay
^[1]

K_D values are measured by fluorescence polarization measurements. For direct titrations, increasing amounts of PDEδ are added to a solution containing 50-100 nM labelled small molecule in 200 µL PBS buffer. For displacement titrations, increasing amounts of the small molecules in DMSO are directly added to fluorescein-labelled atorvastatin (24 nM) and His6-tagged PDEδ (40 nM) in 200 µL PBS-buffer (containing 0.05% CHAPS, 1% DMSO), keeping the concentration of fluorescein-labelled atorvastatin, PDEδ and DMSO constant. For K_D measurements using isothermal titration calorimetry, PDEδ protein (280 µM) is titrated to small molecule (30 µM) in Tris/HCl buffer (temperature 25°C). In the Tm shift assays, protein melting points are detected by circular dichroism spectroscopy in the presence of small molecules.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O / DMSO	1 mM	1.5620 mL	7.8098 mL	15.6196 mL	39.0491 mL
	5 mM	0.3124 mL	1.5620 mL	3.1239 mL	7.8098 mL
	10 mM	0.1562 mL	0.7810 mL	1.5620 mL	3.9049 mL
	15 mM	0.1041 mL	0.5207 mL	1.0413 mL	2.6033 mL
	20 mM	0.0781 mL	0.3905 mL	0.7810 mL	1.9525 mL
	25 mM	0.0625 mL	0.3124 mL	0.6248 mL	1.5620 mL
	30 mM	0.0521 mL	0.2603 mL	0.5207 mL	1.3016 mL
	40 mM	0.0390 mL	0.1952 mL	0.3905 mL	0.9762 mL
	50 mM	0.0312 mL	0.1562 mL	0.3124 mL	0.7810 mL
	60 mM	0.0260 mL	0.1302 mL	0.2603 mL	0.6508 mL
DMSO	80 mM	0.0195 mL	0.0976 mL	0.1952 mL	0.4881 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.