WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H206110
CAS#: 1260612-13-2
Description: SAR260301 is potent and selective Class I phosphatidylinositol-3-kinase (PI3K)β specific inhibitor with an IC50 of 52 nM for this isoform. SAR260301 is being investigated for the treatment of PTEN-deficient tumors. SAR260301 displayed improved physicochemical and in vitro pharmacokinetic properties. SAR260301 demonstrated significant in vivo activity in a UACC-62 xenograft model in mice, warranting further preclinical investigation.
Hodoodo Cat#: H206110
Name: SAR260301
CAS#: 1260612-13-2
Chemical Formula: C19H22N4O3
Exact Mass: 354.17
Molecular Weight: 354.403
Elemental Analysis: C, 64.39; H, 6.26; N, 15.81; O, 13.54
Synonym: SAR260301; SAR260301; SAR 260301.
IUPAC/Chemical Name: (S)-2-(2-(2-methylindolin-1-yl)-2-oxoethyl)-6-morpholinopyrimidin-4(3H)-one
InChi Key: UAXHPOBBKRWJGA-ZDUSSCGKSA-N
InChi Code: InChI=1S/C19H22N4O3/c1-13-10-14-4-2-3-5-15(14)23(13)19(25)11-16-20-17(12-18(24)21-16)22-6-8-26-9-7-22/h2-5,12-13H,6-11H2,1H3,(H,20,21,24)/t13-/m0/s1
SMILES Code: O=C1NC(CC(N2[C@@H](C)CC3=C2C=CC=C3)=O)=NC(N4CCOCC4)=C1
Appearance: white solid powder
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: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
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:
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| In vitro activity: | |
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The following data is based on the product molecular weight 354.40 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: Certal V, Carry JC, Halley F, Virone-Oddos A, Thompson F, Filoche-Rommé B, El-Ahmad Y, Karlsson A, Charrier V, Delorme C, Rak A, Abecassis PY, Amara C, Vincent L, Bonnevaux H, Nicolas JP, Mathieu M, Bertrand T, Marquette JP, Michot N, Benard T, Perrin MA, Lemaitre O, Guerif S, Perron S, Monget S, Gruss-Leleu F, Doerflinger G, Guizani H, Brollo M, Delbarre L, Bertin L, Richepin P, Loyau V, Garcia-Echeverria C, Lengauer C, Schio L. Discovery and optimization of pyrimidone indoline amide PI3Kβ inhibitors for the treatment of phosphatase and tensin homologue (PTEN)-deficient cancers. J Med Chem. 2014 Feb 13;57(3):903-20. doi: 10.1021/jm401642q. Epub 2014 Jan 15. PubMed PMID: 24387221.
