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EHT 1864 is a inhibitor of Rac family GTPases. Blocks activation by direct binding to Rac1, Rac1b, Rac2 and Rac3 (KD values are 40, 50, 60 and 250 nM respectively). Inhibits Rac, Ras and Tiam-induced growth transformation of NIH-3T3 fibroblasts.
EHT 1864 reduces β-amyloid peptide production in vivo. EHT 1864 (oral administration) displays good tolerability, brain penetrance, and no genotoxicity. EHT 1864 (10 and 40 mg/kg/day; daily; 15 days; intraperitoneal injections) lowers brain Aβ 40 by 37% in guinea pigs.
| Molecular Weight | 581.47 |
| Formula | C25H27F3N2O4S.2HCl |
| CAS Number | 754240-09-0 |
| Solubility (25°C) | Water ≥ 90 mg/mL DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Ras Products |
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| AMG410
AMG410 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 is a dual GTP(on)- and GDP(off)-state inhibitor (Kd(GDP-state) of 1 nM; Kd(GTP-state) of 22 nM). AMG410 blocks KRAS signaling in a cycling state-independent manner and also blocks proliferation in wildtype KRAS-amplified tumor cells. |
| HRS-4642
HRS-4642 is a selective KRAS(G12D) inhibitor, with Kd value of 0.083 nM. HRS-4642 has anti-cancer activity. HRS-4642 exhibits significant in vivo potency. |
| AZD0022
AZD0022 is a selective and orally active KRASG12D inhibitor. |
| HH0043
HH0043 is an orally active and potent SOS1 inhibitor, with IC50 value of 5.8 nM. |
| BI-2493
BI-2493 is a structural analogue of BI-2865 and a highly selective and orally active pan-KRAS inhibitor. |
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Products are for research use only. Not for human use. We do not sell to patients.
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