2. Immunology/Inflammation Protein Tyrosine Kinase/RTK
  3. IRAK FLT3
  4. Emavusertib hydrochloride

Emavusertib hydrochloride  (Synonyms: CA-4948 hydrochloride)

Cat. No.: HY-135317B
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Emavusertib (CA-4948) hydrochloride is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib hydrochloride has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib hydrochloride shows anti-tumor activity.

For research use only. We do not sell to patients.

Emavusertib hydrochloride Chemical Structure

Emavusertib hydrochloride Chemical Structure

CAS No. : 2376399-42-5

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Emavusertib hydrochloride Related Antibodies

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Description

Emavusertib (CA-4948) hydrochloride is a selective, potent and orally active IRAK4/FLT3 inhibitor. Emavusertib hydrochloride has an IC50 of 57 nM for IRAK4 in a FRET kinase assay. Emavusertib hydrochloride shows anti-tumor activity[1][2][3].

IC50 & Target

IRAK4

57 nM (IC50)

In Vitro

Emavusertib exhibits >350-fold higher binding affinity for IRAK-4 than that observed for IRAKs 1, 2 and 3[3].
Emavusertib (10 μM, 72 h) decreases the percentage of proliferating cells and induces a moderate increase in the sub-G0 fraction in marginal zone lymphomas (MZL) cell lines[3].
Emavusertib (10 μM, 72 h) induces a significant increase in the apoptotic cell population of MZL cells, particularly when combined with Ibrutinib (HY-10997) compared to ibrutinib and emavusertib alone[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Emavusertib hydrochloride Related Antibodies
In Vivo

Emavusertib (25-150 mg/kg, Orally, once daily, for 14 consecutive days) induces tumor growth inhibition in mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice bearing OCI-LY10 tumors[3]
Dosage: 25, 50, or 150 mg/kg (once daily), 12.5, 25, or 50 mg/kg (twice daily)
Administration: Orally, once daily or twice daily, for 14 consecutive days
Result: Induced tumor growth inhibition. Emavusertib administered as a twice-daily divided dose was equivalent to the corresponding once-daily dose with regards to antitumor activity, i.e., 12.5 mg/kg BID versus 25 mg/kg QD.
Molecular Weight

527.96

Formula

C24H26ClN7O5
CAS No.
SMILES

O=C(C1=COC(C2=CC=NC(C)=C2)=N1)NC3=C(N4CC[C@H](C4)O)N=C5C(OC(N6CCOCC6)=N5)=C3.Cl
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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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Emavusertib hydrochloride Related Classifications

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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.

Keywords:

Emavusertib2376399-42-5CA-4948CA4948CA 4948IRAKFLT3Interleukin-1 receptor associated kinaseIL-1R associated kinaseCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3inflammationMyd88rheumatoidarthritisTollIL-1RlymphomaInhibitorinhibitorinhibit

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