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Synonyms:
AMG410 diTFA
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | AMG410 diTFA is a non-covalent selective pan-KRAS inhibitor with IC50 values of 1-4 nM for KRAS G12D, KRAS G12V, and KRAS G13D. It exhibits over 100-fold selectivity for HRAS and NRAS. AMG410 diTFA is a dual inhibitor of both GTP (active) and GDP (inactive) states, with Kd values of 1 nM for the GDP state and 22 nM for the GTP state. The compound effectively blocks KRAS signaling without dependence on the cycling state and inhibits the proliferation of tumor cells with wild-type KRAS amplification. It is applicable for research in colorectal, pancreatic, and lung cancers. |
| Targets & IC50 | KRas (G12D):1-4 nM |
| In vitro | AMG410 diTFA exhibits potent antiproliferative activity in KRAS mutant cells (median IC 50 = 12 nM). Importantly, AMG410 diTFA does not show antiproliferative activity in non-KRAS transformed cells (median IC 50 > 5 µM). |
| In vivo | AMG410 diTFA demonstrates significant in vivo efficacy by consistently reducing phosphorylated ERK levels throughout the dosing period. It causes tumor stasis or regression in various cell-derived xenograft (CDX) and patient-derived xenograft (PDX) models originating from colorectal, pancreatic, and lung cancer cell lines harboring multiple KRAS mutant alleles, such as G12D, G12V, G12C, and G13D. |
| Molecular Weight | 884.13 |
| Formula | C35H34ClF8N7O9 |
| Cas No. | 3040175-18-3 |
| Smiles | OC(C(F)(F)F)=O.FC1=C2C3=CN=C1C4=C(CCCOC(O[C@@]5([H])CN(CCOC5)C3=NC(OC[C@@]67N(CCC7)C[C@@H](C6)F)=N2)=O)C(Cl)=CC8=C4C=NN8.OC(C(F)(F)F)=O |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 µL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
| Size | Quantity | Unit Price | Amount | Operation |
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