1. PI3K/Akt/mTOR
  2. PI3K
  3. AM-1430

AM-1430 is an efficient, highly selective and orally active small molecule inhibitor of PI3Kδ with an IC50 of 4.6 nM. AM-1430 exhibits IC50s for PI3Kα, PI3Kβ and PI3Kγ of 14.18, 2.2 and 3.22 μM, respectively. AM-1430 inhibits B cell proliferation and exhibits excellent in vivo activity in pAKT inhibition models and the hemoglobin (KLH) immune response model. AM-1430 can be used for the study of inflammation and autoimmune diseases.

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AM-1430

AM-1430 Chemical Structure

CAS No. : 1975263-74-1

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Description

AM-1430 is an efficient, highly selective and orally active small molecule inhibitor of PI3Kδ with an IC50 of 4.6 nM. AM-1430 exhibits IC50s for PI3Kα, PI3Kβ and PI3Kγ of 14.18, 2.2 and 3.22 μM, respectively. AM-1430 inhibits B cell proliferation and exhibits excellent in vivo activity in pAKT inhibition models and the hemoglobin (KLH) immune response model. AM-1430 can be used for the study of inflammation and autoimmune diseases[1].

IC50 & Target[1]

PI3Kδ

4.6 nM (IC50)

PI3Kα

14.18 μM (IC50)

PI3Kβ

2.2 μM (IC50)

PI3Kγ

3.22 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
B cell IC50
0.2 nM
Compound: 7; AM-1430
Inhibition of cell proliferation of human B cells pre-incubated for 30 mins before anti-IgM/CD40L stimulation and measured after 72 hrs by [3H]thymidine incorporation assay
Inhibition of cell proliferation of human B cells pre-incubated for 30 mins before anti-IgM/CD40L stimulation and measured after 72 hrs by [3H]thymidine incorporation assay
[PMID: 27411843]
Sf9 IC50
14180 nM
Compound: 7; AM-1430
Inhibition of polyHis tagged full length recombinant PI3Kalpha (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
Inhibition of polyHis tagged full length recombinant PI3Kalpha (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
[PMID: 27411843]
Sf9 IC50
2200 nM
Compound: 7; AM-1430
Inhibition of polyHis tagged full length recombinant PI3Kbeta (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
Inhibition of polyHis tagged full length recombinant PI3Kbeta (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
[PMID: 27411843]
Sf9 IC50
4.6 nM
Compound: 7; AM-1430
Inhibition of polyHis tagged full length recombinant PI3Kdelta (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
Inhibition of polyHis tagged full length recombinant PI3Kdelta (unknown origin) expressed in Sf9 cells co-expressing p85 incubated for 20 mins by alpha screen assay
[PMID: 27411843]
Molecular Weight

442.45

Formula

C23H19FN8O

CAS No.
SMILES

CNC(C1=C(C([C@@H](NC2=NC=NC(N)=C2C#N)C)=NC3=CC=CC(F)=C13)C4=NC=CC=C4)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
AM-1430
Cat. No.:
HY-115814
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