Pan-RAS-IN-1

SKU: orb1307914

Description

Pan-RAS-IN-1

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 1835283-94-7
• MW: 717.65
• Purity: 99.77%
• Formula: C₃₆H₄₁Cl₂F₃N₆O₂
• SMILES: NC1(CCNCC1)C(=O)NCCCn1cc(-c2ccc(OC(F)(F)F)cc2)c2cc(CN3CCN(Cc4c(Cl)cccc4Cl)CC3)ccc12
• Target: Ras,MAPK
• Solubility: DMSO:50 mg/mL (69.67 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (2.79 mM)

Bioactivity

• In Vivo:
  Pan-RAS-IN-1-treated mice show decreased tumor pERK levels compared with vehicle-treated mice. Pan-RAS-IN-1 administration causes inhibition of tumor growth over 15 days of treatment. A modest increase in cleaved caspase-3 is also observed, showing that pan-RAS-IN-1 has the capacity to induce caspase activation in this model.
• In Vitro:
  Pan-RAS-IN-1 is cytostatic, possibly due to pan-RAS inhibition at some concentrations. Pan-RAS-IN-1 is evaluated in primary T cell acute lymphoblastic leukemia (T-ALL) cells. Selective lethality is observed, with mutant NRAS cells retaining only 20%-40% viability after 5 μM treatment. Pan-RAS-IN-1 binds to KRasG12D-GppNHp with an affinity of less than 20 μM. Pan-RAS-IN-1 binds to Ras proteins and exhibits lethality in cells partially dependent on the expression of Ras proteins. The potency of pan-RAS-IN-1 correlates with the degree of dependency on the mutated isoform over a 5-fold concentration range .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, MAPK, PanRASIN1, Pan-RAS-IN-1, Pan RAS IN 1, inhibit, Ras

Compound Identifiers

PubChem CID

102004330