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| Cas No.: | 1639417-53-0 |
| Synonyms: | RP-6530; RP 6530; RP6530 |
| SMILES: | O=C1C(C2=CC=CC(F)=C2)=C([C@@H](NC3=C4NC=NC4=NC=N3)CC)OC5=CC=CC=C15 |
| Formula: | C23H18FN5O2 |
| M.Wt: | 415.42 |
| Purity: | >98% |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | Tenalisib shows selectivity over PI3K α (>300-fold) and β (>100-fold) isoforms. Tenalisib exhibits modest proliferation inhibition (33-46% inhibition @ 10 μM) in both HEL-RS and HEL-RR cells. Addition of 10 μM tenalisib to ruxolitinib is synergistic resulting in a near-complete inhibition of proliferation (>90% for HEL-RS and >70% for HEL-RR). Addition of 5 μM tenalisib, 4 h prior to the addition of ruxolitinib results in a significant reduction in EC50of ruxolitinib (5.8 μM) in HEL-RR cells. Incubation of 10 μM tenalisib with ruxolitinib for 72 h increases the percent of apoptotic cells (55% in HEL-RS and 37% in HEL-RR) compared to either agent alone (16-27% in HEL-RS and 17-21% in HEL-RR).Tenalisib has been well tolerated in subjects with heavily pre-treated relapsed/refractory hematologic malignancies. Reported toxicities are manageable with no DLTs. Single agent activity is evident in difficult-to-treat subjects at ≥ 200 mg BID. |
MSDS
COA
| LOT NO. | DOWNLOAD |
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| 2018-0101 |
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