WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206612
Description: AM-1430 is a potent and selective PI3Kδ inhibitor. AM-1430 has cellular potency: pAKT IC50 = 0.8 nM; HWB,u (pAKT) IC 50 = 7.7 nM. Rat KLH: IgG ED50 -= 0.016 mg/kg; IhM ED50 = 0.015 mg/kg. Rat PK Clu = 1.7 L/hr/kg. AM-1430 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.
MedKoo Cat#: 206612
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
This product is not in stock, which may be available by custom synthesis.
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Synonym: AM-1430; AM 1430; AM1430.
IUPAC/Chemical Name: 2‑((1S)‑1-((6-Amino-5-cyano-4-pyrimidinyl)amino)ethyl)-5-fluoro‑N‑methyl-3-(2-pyridinyl)-4-quinolinecarboxamide
InChi Key: CCLUQQJLBVGECO-LBPRGKRZSA-N
InChi Code: InChI=1S/C23H19FN8O/c1-12(31-22-13(10-25)21(26)29-11-30-22)20-18(15-7-3-4-9-28-15)19(23(33)27-2)17-14(24)6-5-8-16(17)32-20/h3-9,11-12H,1-2H3,(H,27,33)(H3,26,29,30,31)/t12-/m0/s1
SMILES Code: CNC(C1=C(C2=NC=CC=C2)C([C@H](C)NC3=NC=NC(N)=C3C#N)=NC4=CC=CC(F)=C14)=O
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
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.
|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.
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.