| Identification | Back Directory | [Name]
Tenalisib | [CAS]
1639417-53-0 | [Synonyms]
RP6530
Tenalisib
RP6530, Tenalisib
Tenalisib (RP6530)
RP-6530; RP 6530; RP6530
Tenalisib (Synonyms: RP6530)
4H-1-Benzopyran-4-one, 3-(3-fluorophenyl)-2-[(1S)-1-(9H-purin-6-ylamino)propyl]- | [Molecular Formula]
C23H18FN5O2 | [MOL File]
1639417-53-0.mol | [Molecular Weight]
415.42 |
| Chemical Properties | Back Directory | [Boiling point ]
706.1±60.0 °C(Predicted) | [density ]
1.434±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : ≥ 100 mg/mL (240.72 mM) | [form ]
Solid | [pka]
10.06±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively. | [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]. | [IC 50]
PI3Kδ: 25 nM (IC50); PI3Kγ: 33 nM (IC50) | [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; |
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