AM-0687

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

MedKoo CAT#: 206613

CAS#: 1259522-94-5

Description: 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

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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: 442.4584
Elemental Analysis: C, 62.44; H, 4.33; F, 4.29; N, 25.33; O, 3.62

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

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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

Preparing Stock Solutions

The following data is based on the product molecular weight 442.4584 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

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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.



Additional Information

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.