IACS-010759 HCl
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1250 | Check With Us |
| 500mg | $1950 | Check With Us |
| 1g | $2925 | Check With Us |
: Cat #: V3751 CAS #: 1807523-99-4 Purity ≥ 98%
Description: IACS-10759 HCl (IACS10759; IACS-010759) was identified as a potent and orally bioavailable inhibitor of complex I of oxidative phosphorylation (OXPHOS) with anticancer activity.
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| Molecular Weight (MW) | 599.03 |
|---|---|
| Molecular Formula | C25H26ClF3N6O4S |
| CAS No. | 1807523-99-4 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: > 60 mg/mLr |
| Water: N/Ar | |
| Ethanol: N/A | |
| SMILES Code | FC(F)(F)OC1=CC=C(C2=NOC(C3=NN(CC4=CC=CC(N5CCC(S(=O)(C)=O)CC5)=C4)C(C)=N3)=N2)C=C1.[H]Cl |
| Synonyms | IACS010759 hydrochloride; IACS-010759; IACS 010759; IACS-10759 HCl; IACS 10759; IACS10759 HCl |
| Protocol | In Vitro | IACS-010759 hydrochloride (0.01-10 μM) yieldes a maximal reduction of growth of > 50% in the majority of cancer cell lines (24 of 30 pancreatic (PDAC), 19 of 20 ovarian, 13 of 16 triple-negative breast (TNBC), 8 of 10 non-small-cell lung (NSCLC)) and a subset (11of 30 PDAC, 10 of 20 ovarian, 5 of 16 TNBC, 2 of 10 NSCLC) exhibited > 100% growth inhibition. IACS-010759 hydrochlorideis similarly active in mouse (average IC50 = 5.6 nM), rat (IC50 = 12.2 nM), and cynomolgus monkey (IC50 = 8.7 nM) cell lines. IACS-010759 hydrochloride (0.001, 0.01, 0.1, 1, 10, 100, 1000 nM; 72 hurs) robustly inhibits both OCR and galactose-dependent H460 cell viability and has nearly identical IC50 values of 1.4 nM. IACS-010759 hydrochloride (10, 30, 100 nM; for 4 or 5 days) reduces viability and induces apoptosis in primary AML. |
|---|---|---|
| In Vivo | IACS-010759 hydrochloride (0.3 mg/kg for iv; 1 mg/kg for oral) has low plasma clearance with a high volume of distribution, resulting in a prolonged terminal half-life (>24 h). IACS-010759 HCl (10 mg/kg; orally; QD (daily) or QD×5 (5 d on/2 d off); for 35 d) increases median survival from 28 d to longer than 60 d, whereas less-frequent dosing schedules (Q2D or Q3D) enhances survival to a lesser extent. IACS-010759 hydrochloride (5, 10, 25 mg/kg/day; oral; for 21 d) results in tumor regression with minimal body weight loss at the 5 or 10 mg/kg dose in mice bearing NB-1 (PGD-null) subcutaneous xenografts. IACS-010759 at the 25 mg/kg dose is not tolerated. |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.6694 mL | 8.3468 mL | 16.6937 mL | 33.3873 mL |
| 5mM | 0.3339 mL | 1.6694 mL | 3.3387 mL | 6.6775 mL |
| 10mM | 0.1669 mL | 0.8347 mL | 1.6694 mL | 3.3387 mL |
| 20mM | 0.0835 mL | 0.4173 mL | 0.8347 mL | 1.6694 mL |
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