<Suppliers Price>

Tenalisib

Names

[ CAS No. ]:
1639417-53-0

[ Name ]:
Tenalisib

[Synonym ]:
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

Biological Activity

[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;


[Related Small Molecules]

3-Methyladenine | LY294002 | Wortmannin | Alpelisib (BYL719) | BKM120 | Eganelisib(IPI-549) | BAY 80-6946 (Copanlisib) | Idelalisib (CAL-101) | Dactolisib (BEZ235) | Quercetin | SAR-405 | GDC-0941 | 740 Y-P | LY3023414 | 1,3-Dicaffeoylquinic acid

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

[ Storage condition ]:
-20℃


Related Compounds