MEK/PI3K-IN-1

SKU:BHB21901208
Overview
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MEK/PI3K-IN-1 (CAS 2281803-28-7) is an inhibitor. Reported to act on MEK1, PI3Kα, PI3Kδ. Relevant to MAPK/ERK Pathway and PI3K/Akt/mTOR research. Molecular formula C36H37F5IN9O6, molecular weight 913.63 g/mol.
CAS Number 2281803-28-7
Molecular Weight 913.63 g/mol
Target MEK1, PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ
Storage See Certificate of Analysis
Options selector
Catalog no. Size
HY-144692-50MG 50 mg
HY-144692-100MG 100 mg
HY-144692-250MG 250 mg
Available Options

Select the variant that best fits your experiment. Availability and lead time may vary by option.

  • Options: Size: 50 mg, 100 mg, 250 mg
  • Lead time: confirmed on inquiry for every option.
  • Storage: Please store the product under the recommended conditions in the Certificate of Analysis.
  • Shipping: Room temperature in continental US; may vary elsewhere.
  • Upon receipt: store as stated on the Certificate of Analysis; contact us if you need the condition before ordering.
Field Specification
Target MEK1, PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ
CAS no. 2281803-28-7
Applications
  • Functional Assay (In Vitro)
Molecular weight 913.63
Molecular formula C36H37F5IN9O6
SMILES O=C(C1=C(C(F)=C(C=C1)F)NC2=CC=C(C=C2F)I)NOCCOCCOCCOCCNC3=NC(N4CCOCC4)=NC(N5C(C(F)F)=NC6=C5C=CC=C6)=N3
Storage Refer to Certificate of Analysis (CoA) for storage conditions
Shipping Room temperature in continental US; may vary elsewhere.
Catalog no. (Mfr.) HY-144692
Main SKU BHB21901208
Inhibitors

Compound Overview

MEK/PI3K-IN-1 is a potent MEK/PI3K inhibitor with IC50 values of 124 nM against MEK1, 130 nM against PI3Kα, and 236 nM against PI3Kδ. It suppresses pAKT and pERK1/2 levels and displays anti-proliferative activity against tumor cell lines[1]. It has a molecular formula of C36H37F5IN9O6 and a molecular weight of 913.63 g/mol.

Physical & Chemical Properties

CAS Number 2281803-28-7
Molecular Formula C36H37F5IN9O6
Molecular Weight 913.63 g/mol
SMILES O=C(C1=C(C(F)=C(C=C1)F)NC2=CC=C(C=C2F)I)NOCCOCCOCCOCCNC3=NC(N4CCOCC4)=NC(N5C(C(F)F)=NC6=C5C=CC=C6)=N3
Target MEK1, PI3Kα, PI3Kδ, PI3Kβ, PI3Kγ
Signaling Pathway MAPK/ERK Pathway; PI3K/Akt/mTOR; Cell Cycle/DNA Damage
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping Room temperature in continental US; may vary elsewhere.

Biological Activity

IC50 & Target

MEK1

124 ± 11 nM (IC50)

PI3Kα

130 ± 13 nM (IC50)

PI3Kδ

236 ± 29 nM (IC50)

PI3Kβ

1537 ± 188 nM (IC50)

PI3Kγ

2745 ± 485 nM (IC50)

Literature Cited

Sources cited in this description. Peer-reviewed publications that used this product are listed under References.

[1]. Van Dort ME, et al. Structural effects of morpholine replacement in ZSTK474 on Class I PI3K isoform inhibition: Development of novel MEK/PI3K bifunctional inhibitors. Eur J Med Chem. 2022 Feb 5;229:113996.

Safety

For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.

Q.Why is there no price listed?
A.Every size of this product is quoted on inquiry. Send us the size you need and we will come back with price and lead time.
Q.Can this be used in humans or for diagnostics?
A.No. This product is supplied For Research Use Only. It is not for diagnostic or therapeutic procedures and not for human or veterinary use.

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