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

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).

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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.

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