MRTX-EX185

Cat. No.: HY-145962: Data Sheet
SDS
Handling Instructions
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MRTX-EX185 is a potent KRAS (G12D) inhibitor with an IC₅₀ of 90 nM. MRTX-EX185 can binds both GDP-loaded and active GNP states of KRAS and KRAS (G12D). MRTX-EX185 exhibits broad-spectrum binding properties with IC₅₀s of 110, 290, 130 and 240 nM for KRAS WT, KRAS (G12C), KRAS (Q61H), KRAS (G13D). MRTX-EX185 also binds GDP-loaded HRAS. MRTX-EX185 can be used to study various RAS-driven tumors (such as pancreatic cancer) .

The free form of the compound is prone to instability, it is advisable to consider the stable salt form (MRTX-EX185 formic) that retains the same biological activity.

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

MRTX-EX185 Chemical Structure

CAS No. : 2621927-57-7

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This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of MRTX-EX185:

MRTX-EX185 formic

Other Forms of MRTX-EX185:

MRTX-EX185 formic In-stock

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K-Ras H-Ras N-Ras Ras

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

KRas G12D

90 nM (IC₅₀)

K-Ras WT

110 nM (IC₅₀)

KRas G12C

290 nM (IC₅₀)

KRas G12V

700 nM (IC₅₀)

KRAS G13D

240 nM (IC₅₀)

KRas Q61H

130 nM (IC₅₀)

In Vitro

MRTX-EX185 (0.1 nM-100 μM) suppresses cell proliferation (IC₅₀ = 70 nM) in KRAS (G12D)-driven SW-1990 pancreatic cancer cells, and is non-toxic to non-KRAS-dependent cell lines (HEK293 cells)^[1].
MRTX-EX185 (1 nM-100 μM) significantly inhibits ERK phosphorylation (p-ERK) in KRAS(G12C)-driven cell lineages^[1].

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

Molecular Weight

564.65

Formula

C₃₃H₃₃FN₆O₂

CAS No.

2621927-57-7

Appearance

Solid

Color

Light brown to brown

SMILES

OC1=CC(C2=C(F)C3=NC(OCC45CCCN4CCC5)=NC(N6C[C@@](N7)([H])CC[C@@]7([H])C6)=C3C=N2)=C8C(C#C)=CC=CC8=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Data Sheet (273 KB) SDS (252 KB) Handling Instructions (2659 KB)

References

[1]. Vasta JD, et, al. KRAS is vulnerable to reversible switch-II pocket engagement in cells. Nat Chem Biol. 2022 Mar 21. [Content Brief]

MRTX-EX185 Related Classifications

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

Mass		Concentration		Volume		Molecular Weight *
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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MRTX-EX1852621927-57-7RasGDP-loadedKRAS(G12D)HRASInhibitorinhibitorinhibit

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