MedKoo Cat#: 206613 | Name: AM-0687

Description:

WARNING: This product is for research use only, not for human or veterinary use.

AM-0687 is a potent and selective PI3Kδ inhibitor. AM-0687 has Cellular potency: pAKT IC50 = 0.7 nM; HWB, u (pAKT) IC 50 = 4.6 nM. Rat KLH: IgG ED50 -= 0.026 mg/kg; IgM ED50 = 0.016 mg/kg. Rat PK Clu = 2.3 L/hr/kg. AM-0687 displays excellent potency and selectivity profile in biochemical and cellular assays as well as optimal rat PK profile. PI3Kδ is hyperactivated in B-cell malignancies and plays a vital role in the B-cell receptor pathway, a key oncogenic driver in various B-cell malignancies, including CLL.

Chemical Structure

AM-0687
AM-0687
CAS#1259522-94-5

Theoretical Analysis

MedKoo Cat#: 206613

Name: AM-0687

CAS#: 1259522-94-5

Chemical Formula: C23H19FN8O

Exact Mass: 442.1666

Molecular Weight: 442.46

Elemental Analysis: C, 62.44; H, 4.33; F, 4.29; N, 25.33; O, 3.62

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
AM-0687; AM 0687; AM0687.
IUPAC/Chemical Name
2‑((1S)‑1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro‑N‑methyl-3-(2-pyridinyl)-4-quinolinecarboxamide
InChi Key
OLJXUPJOUSFYSX-LBPRGKRZSA-N
InChi Code
InChI=1S/C23H19FN8O/c1-12(31-22-15(10-25)21(26)29-11-30-22)20-19(17-5-3-4-8-28-17)18(23(33)27-2)14-9-13(24)6-7-16(14)32-20/h3-9,11-12H,1-2H3,(H,27,33)(H3,26,29,30,31)/t12-/m0/s1
SMILES Code
O=C(C1=C(C2=NC=CC=C2)C([C@@H](NC3=NC=NC(N)=C3C#N)C)=NC4=CC=C(F)C=C14)NC
Appearance
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
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
Note: Idelalisib is a potent, first-in-class selective inhibitor of phosphatidylinositol-3-kinaseδ (PI3Kδ) approved by the FDA in July 2014 for the treatment of relapsed CLL, in combination with rituximab, in patients for whom rituximab monotherapy would be considered appropriate due to other comorbidities.

Preparing Stock Solutions

The following data is based on the product molecular weight 442.46 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.

Recalculate based on batch purity %
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
1: Gonzalez-Lopez de Turiso F, Hao X, Shin Y, Bui M, Campuzano ID, Cardozo MG, Dunn MC, Duquette J, Fisher B, Foti RS, Henne KR, He X, Hu YL, Kelly RC, Johnson MG, Lucas BS, McCarter JD, McGee LR, Medina JC, Metz DP, San Miguel T, Mohn D, Tran T, Vissinga C, Wannberg S, Whittington DA, Whoriskey J, Yu G, Zalameda L, Zhang X, Cushing TD. Discovery and in Vivo Evaluation of the Potent and Selective PI3Kδ Inhibitors 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-6-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-0687) and 2-((1S)-1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro-N-methyl-3-(2-pyridinyl)-4-quinolinecarboxamide (AM-1430). J Med Chem. 2016 Jul 14. [Epub ahead of print] PubMed PMID: 27411843.