CAS 1639417-53-0|Tenalisib
Introduction：Basic information about CAS 1639417-53-0|Tenalisib, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Tenalisib | ||
|---|---|---|---|
| CAS Number | 1639417-53-0 | Molecular Weight | 415.420 |
| Density | 1.4±0.1 g/cm3 | Boiling Point | / |
| Molecular Formula | C23H18FN5O2 | Melting Point | / |
| MSDS | / | Flash Point | / |
Names
| Name | Tenalisib |
|---|---|
| Synonym | More Synonyms |
Tenalisib BiologicalActivity
| Description | Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively. |
|---|---|
| Related Catalog | Research Areas >>Cancer |
| Target | PI3Kδ:25 nM (IC50) PI3Kγ:33 nM (IC50) |
| In Vitro | 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)[1]. |
| In Vivo | 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[2]. |
| References | [1]. Vakkalanka S, et al. RP6530, a dual PI3K δ/γ inhibitor, potentiates ruxolitinib activity in the JAK2-V617F mutant erythroleukemia cell lines. [abstract]. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research; 2015 Apr 18-22; Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 2704. doi:10.1158/1538-7445.AM2015-2704 [2]. Carmelo C, et al. A Dose Escalation Study of RP6530, a Novel Dual PI3K Delta/Gamma Inhibitor, in Patients with Relapsed/Refractory Hematologic Malignancies. Blood 2015 126:1495; |
Chemical & Physical Properties
| Density | 1.4±0.1 g/cm3 |
|---|---|
| Molecular Formula | C23H18FN5O2 |
| Molecular Weight | 415.420 |
| Exact Mass | 415.144440 |
| LogP | 5.11 |
| Index of Refraction | 1.715 |
| InChIKey | HDXDQPRPFRKGKZ-INIZCTEOSA-N |
| SMILES | CCC(Nc1ncnc2nc[nH]c12)c1oc2ccccc2c(=O)c1-c1cccc(F)c1 |
| Storage condition | -20℃ |
Synonyms
| tenalisib |
| 4H-1-Benzopyran-4-one, 3-(3-fluorophenyl)-2-[(1S)-1-(9H-purin-6-ylamino)propyl]- |
| 2261HH611H |
| 3-(3-Fluorophenyl)-2-[(1S)-1-(9H-purin-6-ylamino)propyl]-4H-chromen-4-one |
