I-7447 Idelalisib, Free Base, >99%

Synonyms : [CAL-101] [GS-1101]

Related Terms : [Zydelig]

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  • 25 mg
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  • 50 mg
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  • 100 mg
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  • 200 mg
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  • 158
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  • 500 mg
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  • 1 g
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  • 2 g
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  • M.W. 415.42
  • C22H18FN7O
  • [870281-82-6]

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  • Idelalisib, also known as CAL-101 or GS-1101, is a selective inhibitor of phosphoinositide 3-kinase (PI3K) P110[delta] with an IC50 of 2.5 nM. It also inhibits other class I PI3Ks including p110[alpha] (IC50 = 820 nM), p110[beta] (IC50 = 565 nM), and p110[gamma] (IC50 = 89 nM). Idelalisib inhibited constitutive PI3K signaling and induced apoptosis in a broad range of immature and mature B-cell malignancies. Lannutti B.J., et al. "CAL-101, a p110delta selective phosphatidylinositol-3-kinase inhibitor for the treatment of B-cell malignancies, inhibits PI3K signaling and cellular viability." Blood 117: 591-594 (2011).
  • Idelalisib showed a unique pattern of response with early lymphocytosis concomitant with reduction in lymph-node and spleen size in patients with chronic lymphocytic leukemia. Byrd J.C., et al. "Translating PI3K-Delta Inhibitors to the Clinic in Chronic Lymphocytic Leukemia: The Story of CAL-101 (GS1101)." Am. Soc. Clin. Oncol. Educ. Book 32: 691-694 (2012).
  • Idelalisib blocked proliferation of LB and INA-6 multiple myeloma (MM) cell lines and patient MM cells, associated with inhibition of Akt phosphorylation. Idelalisib inhibited MM cell growth induced by interleukin-6, insulin-like growth factor-1, and bone marrow stromal cell coculture. Combination of idelalisib and bortezomib induced synergistic cytotoxicity against MM cells. However, idelalisib did not inhibit survival of normal peripheral blood mononuclear cells. Ikeda H., et al. "PI3K/p110{delta} is a novel therapeutic target in multiple myeloma." Blood 116: 1460-1468 (2010).
  • Please note that, as of October 1, 2014, Shanghai Biochempartner is using an incorrect and confusing CAS number for Idelalisib, Free Base. The correct CAS number for Idelasilib, Free Base is given above. The correct CAS number for the compound that this vendor is confusing with Idelasilib is 870281-17-7. This compound differs from Idelalisib by having a methyl group instead of the ethyl group in Idelalisib. The incorrect CAS number being used by this vendor for the methyl analog, 1146702-54-6, has been deleted by Chemical Abstracts Service and is no longer in use.
  • Idelalisib is the active ingredient in the drug product sold under the trade name Zydelig®. This drug is currently approved in at least one country for use in patients with different types of leukemia. NOTE: THE IDELALISIB SOLD BY LC LABORATORIES FOR RESEARCH IS NOT ZYDELIG®, AND IS NOT FOR HUMAN USE.
  • Sold for laboratory or manufacturing purposes only; not for human, veterinary, food, or household use.
  • This product is offered for R&D use in accordance with (i) 35 USC 271(e)+A13(1) in the U.S.; (ii) Section 69.1 of Japanese Patent Law in Japan; (iii) Section 11, No. 2 of the German Patent Act of 1981 in Germany; (iv) Section 60, Paragraph 5b of the U.K. Patents Act of 1977 in the U.K.; (v) Sections 55.2(1) and 55.2(6) and other common law exemptions of Canadian patent law; (vi) Section 68B of the Patents Act of 1953 in New Zealand together with the amendment of same by the Statutes Amendment Bill of 2002; (vii) such related legislation and/or case law as may be or become applicable in the aforementioned countries; and (viii) such similar laws and rules as may apply in various other countries.
  • Not available in some countries; not available to some institutions; not available for some uses.