KRAS inhibitor-10

Name: KRAS inhibitor-10
Brand: MedChemExpress
SKU: HY-138295
Rating: 4.5 (1 reviews)

Cat. No.: HY-138295 Purity: 99.86%: FAQs
Data Sheet SDS COA Handling Instructions

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KRAS inhibitor-10 (compound 11) selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.

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

KRAS inhibitor-10 Chemical Structure

CAS No. : 2578876-75-0

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 495	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 495	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 800	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 2550	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 3900	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

KRas G12C

In Vitro

KRAS inhibitor-10 (0.1-50 µΜ; 72 hours) has antiproliferative effects in KRas mutant tumor cells, KRAS inhibitor-10 is against A549 (lung carcinoma cell line bearing KRas^G12S oncogenic mutation), H358 (non-small cell lung cancer line bearing KRas^G12C oncogenic mutation), PANC-1 (epithelioid carcinoma of the pancreas cell line bearing KRas^G12D oncogenic mutation) and RPMI (myeloma cell line bearing KRas^G12A oncogenic mutation) cell proliferation with IC₅₀ values of 0.2 μM, 0.2 μM, 0.1 μM and 0.8 μM, respectively^[1].
KRAS inhibitor-10 (0-1 μM, 7 days) is against cell viability in a 3D CellTiter-GloTM cell viability assay for NIH-H358 cell, the IC₅₀ value is 0.413 μM^[1].

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

In Vivo

KRAS inhibitor-10 (oral administration; 20 mg/kg; BID; 27 days) is safe and tolerate for the bearing mice. KRAS inhibitor-10 demonstrates significant oral anti-tumor activities in vivo. And the tumor growth inhibition (TGI) value is 48.22% for KRAS inhibitor-10^[1].

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

Animal Model:	Subcutaneous NCI-H358 Human Lung Cancer Model in NCr nude mice^[1]
Dosage:	20 mg/kg
Administration:	Oral administration; 20 mg/kg; BID; 27 days
Result:	Decreased tumor volume and exhibited anti-tumor effects in the bearing mice.

Molecular Weight

519.63

Formula

C₃₀H₃₇N₃O₅

CAS No.

2578876-75-0

Appearance

Solid

Color

White to off-white

SMILES

O=C(N1C(C2=CC=C(OC)C=C2C)C3=C(C=C(OC)C(OCCC4=CC=C(OC)C(N)=C4)=C3)CC1)NCC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (192.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.9244 mL	9.6222 mL	19.2445 mL
5 mM	0.3849 mL	1.9244 mL	3.8489 mL
10 mM	0.1924 mL	0.9622 mL	1.9244 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (4.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.86%

Select Batch:

Data Sheet (272 KB) SDS (251 KB)

COA (247 KB) HNMR (284 KB) LCMS (267 KB)

Handling Instructions (2659 KB)

References

[1]. Miguel VEGA GARCÍA, et al. Tetrahydroisoquinoline compounds. Patent wo2021002165

Complete Stock Solution Preparation Table

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

DMSO	1 mM	1.9244 mL	9.6222 mL	19.2445 mL	48.1112 mL
	5 mM	0.3849 mL	1.9244 mL	3.8489 mL	9.6222 mL
	10 mM	0.1924 mL	0.9622 mL	1.9244 mL	4.8111 mL
	15 mM	0.1283 mL	0.6415 mL	1.2830 mL	3.2074 mL
	20 mM	0.0962 mL	0.4811 mL	0.9622 mL	2.4056 mL
	25 mM	0.0770 mL	0.3849 mL	0.7698 mL	1.9244 mL
	30 mM	0.0641 mL	0.3207 mL	0.6415 mL	1.6037 mL
	40 mM	0.0481 mL	0.2406 mL	0.4811 mL	1.2028 mL
	50 mM	0.0385 mL	0.1924 mL	0.3849 mL	0.9622 mL
	60 mM	0.0321 mL	0.1604 mL	0.3207 mL	0.8019 mL
	80 mM	0.0241 mL	0.1203 mL	0.2406 mL	0.6014 mL
	100 mM	0.0192 mL	0.0962 mL	0.1924 mL	0.4811 mL