5-Fluoro-3-phenyl-2-[1-(9H-purin-6-ylamino)propyl]-4(3H)-quinazolinone(CAS#870281-82-6)

Chemical Property:

Molecular Formula	C22H18FN7O
Molar Mass	415.42
Density	1.47
Melting Point	250-252oC
Boling Point	733.4±70.0 °C(Predicted)
Solubility	DMSO 83 mg/mL Water <1 mg/mL Ethanol 35 mg/mL
Appearance	White solid.
Color	White
pKa	10.00±0.10(Predicted)
Storage Condition	-20°C
Stability	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months.
Use	A potent PI3K p110δ inhibitor
In vitro study	CAL-101 had little effect on p110α, p110β, and p110γ. CAL-101 acts on primary basophils to specifically block the CD63 expression regulated by fcO_c_c_r1 p110δ, with an EC50 of 8 nM. CAL-101 acts on B- cell acute lymphoblastic leukemia (B-ALL) and chronic lymphocytic leukemia (CLL) compared to acute myeloid leukemia (AML) and Myeloproliferative neoplasm (MPN) cells cells showed stronger activity. CAL-101 acts on SU-DHL-5, KARPAS-422 and CCRF-SB cells, reducing pAktS473, pAktT308, and the downstream target S6, EC50 of 0.1 to 1.0 μm. CAL-101 acts on CLL cells, inducing selective cytotoxicity, not through mutational status or interphase cytogenetics, but primarily through a caspase-dependent mechanism. Compared with normal B cells, CAL-101 preferentially produces cytotoxicity on CLL cells, and compared with LY294002, it does not produce toxicity on other hematopoietic cells. CAL-101 act on T cells and natural killer cells lack direct cytotoxic potential. CAL-101 inhibits the production of inflammatory cytokines, such as IL-6, IL-10, TNF-alpha, and IFN-gamma, and activates induced cytokines, such as CD40L. CAL-101 also resisted CD40L regulated CLL cell survival. CAL-101 acts on L1236 and L591 cells to induce cell accumulation in G1 phase and decrease in S phase, indicating that CAL-101 can be used as a new strategy for the treatment of Hodgkin’s lymphoma (HL).

Send email to us

Product Detail

Product Tags

HS Code

29399990

Introduction

CAL-101 (Idelalisib, GS-1101) is a selective p110δ inhibitor with IC50 of 2.5 nM; The selectivity of p110δ acting on p110δ is 40 to 300 times higher than that of p110α/β/γ, and the selectivity of p110δ acting on p110δ is 400 to 4000 times higher than that of C2β, hVPS34, DNA-PK and mTOR. Phase 3.

Application
Idelalisib (CAL-101, GS-1101) is a potent and highly selective small-molecule PI3Kδ inhibitor that functions as an active pharmaceutical ingredient (API) and a specialized research tool for oncology drug discovery. It is indicated for the treatment of relapsed chronic lymphocytic leukemia (CLL), follicular B‑cell non‑Hodgkin lymphoma (FL), and small lymphocytic lymphoma (SLL). By targeting the PI3Kδ isoform (IC₅₀ = 2.5 nM), idelalisib effectively disrupts key B‑cell receptor (BCR) and chemokine signaling pathways, inducing apoptosis of malignant cells and inhibiting chemotaxis and adhesion. This quinazolinone-based compound is widely used in pharmaceutical R&D, serving as a certified reference material for analytical method development (AMD), method validation (AMV), and quality control (QC) in ANDA filings and commercial production. As a versatile building block, it supports drug discovery programs, GMP manufacturing, and preclinical studies for hematologic malignancies. Xinchem offers high‑purity idelalisib with flexible custom synthesis and reliable contract manufacturing, scaled from R&D to commercial tons. Contact us for a competitive quote and reliable global supply.

Previous: Ataluren (PTC124)(CAS#775304-57-9)

Next: 1-(trimethylsilyl)prop-1-yne(CAS#6224-91-5)

analytical reference standard