Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Tenalisib
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Purity: 98.0%
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DC Chemicals Limited
China
Product Name: Tenalisib
Price: $700.0/100mg $1400.0/250mg $2800.0/1g
Purity: 98.0%
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Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Tenalisib
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Purity: 98.0%
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1639417-53-0

1639417-53-0 structure

1639417-53-0 structure

Name: Tenalisib
Chemical Name: Tenalisib
CAS Number: 1639417-53-0
Molecular Formula: C₂₃H₁₈FN₅O₂
Molecular Weight: 415.420
Catalog: Research Areas Cancer
Create Date: 2018-10-17 19:29:57
Modify Date: 2024-01-05 16:19:04
Tenalisib (RP6530) is a novel, potent, and selective PI3Kδ and PI3Kγ inhibitor with IC50 values of 25 and 33 nM, respectively.

Name	Tenalisib
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

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;

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℃