2. GPCR/G Protein MAPK/ERK Pathway
  3. Ras
  4. 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 (Kd(GDP-state) of 1 nM; Kd(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.

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

AMG410 diTFA

AMG410 diTFA Chemical Structure

CAS No. : 3040175-18-3

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AMG410 diTFA Related Antibodies

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Description

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 (Kd(GDP-state) of 1 nM; Kd(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[1][2].

IC50 & Target[1]

KRas G12D

1-4 nM (IC50)

KRas G12V

1-4 nM (IC50)

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.

AMG410 diTFA Related Antibodies
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.
Molecular Weight

884.13

Formula

C35H34ClF8N7O9
CAS No.
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
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
References
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AMG410 diTFA Related Classifications

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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:

AMG410 diTFA3040175-18-3RasKRAS inhibitorRAS G12DKRAS G12Vand KRAS G13Dcolorectalpancreaticand lung cancerInhibitorinhibitorinhibit

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