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Cat. No.: HY-173632A

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AMG410 diTFA

AMG410 diTFA is a non-covalent and selective pan-KRAS inhibitor with IC₅₀ values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. AMG410 diTFA shows greater than 100-fold selectivity against both HRAS and NRAS. AMG410 diTFA is a dual GTP(on)- and GDP(off)-state inhibitor (K_d(GDP-state) of 1 nM; K_d(GTP-state) of 22 nM). AMG410 diTFA blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. AMG410 diTFA can be used for the study of colorectal, pancreatic, and lung cancers.

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CAS No.: 3040175-18-3
Formule: C₃₅H₃₄ClF₈N₇O₉
Masse moléculaire:884.13

Stockage:

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

Data Sheet (279 KB)

AMG410 diTFA Chemical Structure

CAS No.: 3040175-18-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références
Calculators
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Description

IC₅₀ & Target^[1]

KRas G12D

1-4 nM (IC₅₀)

KRas G12V

1-4 nM (IC₅₀)

Voir tous les produits spécifiques à Isoform Ras :

In Vitro

AMG410 diTFA shows potent antiproliferative activity in KRAS-mutant cells (median IC₅₀ = 12 nM). Importantly, AMG410 diTFA does not have antiproliferative activity in non-KRAS-transformed cells (median IC₅₀ > 5 µM)^[1].

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

In Vivo

AMG410 diTFA demonstrates strong in vivo efficacy efficacy, robustly lowing phosphorylated ERK levels throughout dosing cycles and achieving tumor stasis or regression across a broad set of colorectal, pancreatic, and lung cancer cell line-derived xenograft (CDX) and patient-derived xenograft (PDX) models harboring a diverse set of KRAS mutant alleles including G12D, G12V, G12C, & G13D^[1].

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

Chemical Information

CAS No. 3040175-18-3
Masse moléculaire 884.13
Formule C₃₅H₃₄ClF₈N₇O₉
SMILES

FC1=C(C2=C(C=NN3)C3=CC(Cl)=C2CCCO4)N=CC5=C1N=C(OC[C@]67C[C@@H](F)CN6CCC7)N=C5N8CCOC[C@@H](OC4=O)C8.O=C(O)C(F)(F)F.O=C(O)C(F)(F)F
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Adriano BAUER, et al. Macrocyclic kras inhibitors and methods of use. WO2024107686A1.

[2]. Brian A. Lanman, et al. Abstract ND01: AMG 410: An H/NRAS-sparing pan-KRAS inhibitor with dual GTP(on)/GDP(off)-state activity for the treatment of diverse KRAS-mutant tumors. Cancer Res (2025) 85 (8_Supplement_2): ND01.

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Pureté et documentation
Références

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AMG410 diTFA

Voir tous les produits spécifiques à Isoform Ras

Activité biologique

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs

AMG410 diTFA Related Classifications

HY-173632A Related Classifications