WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H124940
CAS#: 2242053-82-1 (mesylate)
Description: CH5132799, also known as PA-799, is a novel class I PI3K inhibitor, which exhibited a strong inhibitory activity especially against PI3Kα (IC(50)=0.014 μM). In human tumor cell lines with PI3K pathway activation, CH5132799 showed potent antiproliferative activity. CH5132799 is orally available and showed significant antitumor activity in PI3K pathway-activated human cancer xenograft models in mice. CH5132799 selectively inhibited class I PI3Ks and PI3Kα mutants in in vitro kinase assays. Tumors harboring PIK3CA mutations were significantly sensitive to CH5132799 in vitro and were remarkably regressed by CH5132799 in in vivo mouse xenograft models.
Hodoodo Cat#: H124940
Name: CH-5132799 Mesylate
CAS#: 2242053-82-1 (mesylate)
Chemical Formula: C16H23N7O6S2
Exact Mass: 473.12
Molecular Weight: 473.520
Elemental Analysis: C, 40.58; H, 4.90; N, 20.71; O, 20.27; S, 13.54
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Related CAS #: 1007207-67-1 (free base) 2242053-82-1 (mesylate)
Synonym: PA-799 mesylate; CH-5132799 Mesilate; CH-5132799 Mesylate; CH5137299 Mesylate; PA 799 mesylate; IZORLISIB MESILATE; IZORLISIB MESYLATE
IUPAC/Chemical Name: 5-(7-(methylsulfonyl)-2-morpholino-6,7-dihydro-5H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrimidin-2-amine methanesulfonate
InChi Key: QASDCQIMDVXWHK-UHFFFAOYSA-N
InChi Code: InChI=1S/C15H19N7O3S.CH4O3S/c1-26(23,24)22-3-2-11-12(10-8-17-14(16)18-9-10)19-15(20-13(11)22)21-4-6-25-7-5-21;1-5(2,3)4/h8-9H,2-7H2,1H3,(H2,16,17,18);1H3,(H,2,3,4)
SMILES Code: CS(O)(=O)=O.CS(=O)(=O)N1CCC2=C(N=C(N=C12)N3CCOCC3)C4=CN=C(N)N=C4
Appearance: To be determined
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: To be determined
Shelf Life: >2 years if stored properly
Drug Formulation: To be determined
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 473.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Correction: First-in-Human Study of CH5132799, an Oral Class I PI3K Inhibitor, Studying Toxicity, Pharmacokinetics, and Pharmacodynamics, in Patients with Metastatic Cancer. Clin Cancer Res. 2015 Feb 1;21(3):660. doi: 10.1158/1078-0432.CCR-14-3188. PubMed PMID: 25646183.
2: Blagden S, Omlin A, Josephs D, Stavraka C, Zivi A, Pinato DJ, Anthoney A, Decordova S, Swales K, Riisnaes R, Pope L, Noguchi K, Shiokawa R, Inatani M, Prince J, Jones K, Twelves C, Spicer J, Banerji U. First-in-human study of CH5132799, an oral class I PI3K inhibitor, studying toxicity, pharmacokinetics, and pharmacodynamics, in patients with metastatic cancer. Clin Cancer Res. 2014 Dec 1;20(23):5908-17. doi: 10.1158/1078-0432.CCR-14-1315. Epub 2014 Sep 17. Erratum in: Clin Cancer Res. 2015 Feb 1;21(3):660. Olmin, Aurelius [corrected to Omlin, Aurelius]. PubMed PMID: 25231405; PubMed Central PMCID: PMC4254850.
3: Tanaka H, Yoshida M, Tanimura H, Fujii T, Sakata K, Tachibana Y, Ohwada J, Ebiike H, Kuramoto S, Morita K, Yoshimura Y, Yamazaki T, Ishii N, Kondoh O, Aoki Y. The selective class I PI3K inhibitor CH5132799 targets human cancers harboring oncogenic PIK3CA mutations. Clin Cancer Res. 2011 May 15;17(10):3272-81. doi: 10.1158/1078-0432.CCR-10-2882. Epub 2011 May 10. PubMed PMID: 21558396.
4: Ohwada J, Ebiike H, Kawada H, Tsukazaki M, Nakamura M, Miyazaki T, Morikami K, Yoshinari K, Yoshida M, Kondoh O, Kuramoto S, Ogawa K, Aoki Y, Shimma N. Discovery and biological activity of a novel class I PI3K inhibitor, CH5132799. Bioorg Med Chem Lett. 2011 Mar 15;21(6):1767-72. doi: 10.1016/j.bmcl.2011.01.065. Epub 2011 Jan 22. PubMed PMID: 21316229.