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CA-4948

SKU: orb1298434

Description

CA-4948 (Emavusertib) is a small molecule inhibitor targeting IRAK4 and FLT3 kinases. It has demonstrated anti-tumor activity in preclinical research, showing efficacy in both in vitro cellular assays and in vivo models of hematological malignancies.

Research Area

Cardiovascular Research, Cell Biology, Immunology & Inflammation, Signal Transduction

Images & Validation

Key Properties

CAS Number1801344-14-8
MW491.5
Purity99.88% (May vary between batches)
FormulaC24H25N7O5
SMILESCc1cc(ccn1)-c1nc(co1)C(=O)Nc1cc2oc(nc2nc1N1CC[C@@H](O)C1)N1CCOCC1
TargetNF-κB,Apoptosis,IRAK,FLT,MyD88
Solubility10% DMSO+40% PEG300+5% Tween-80+45% Saline:2 mg/mL (4.07 mM);H2O:< 0.1 mg/mL (insoluble);DMSO:27.78 mg/mL (56.52 mM)

Bioactivity

In Vitro
CA-4948, demonstrated good cellular activity in ABC DLBCL and AML cell lines. Inhibition of TLR signaling leading to decreased IL-6 levels was also observed in whole blood assays. CA-4948 demonstrated moderate to high selectivity in a panel of 329 kinases as well as exhibited desirable ADME and PK profiles including good oral bioavailability in mice, rat, and dog and showed >90% tumor growth inhibition in relevant tumor models with excellent correlation with in vivo PD modulation. CA-4948 was well tolerated in toxicity studies in both mouse and dog at efficacious exposure. The overall profile of CA-4948 prompted us to select it as a clinical candidate for evaluation in patients with relapsed or refractory hematologic malignancies including non-Hodgkin lymphoma and acute myeloid leukemia.

Storage & Handling

Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Cluster of differentiation antigen 135, CD135, CA 4948, CA-4948, CA4948, arthritis, Inhibitor, FLT3, Fms like tyrosine kinase 3, Emavusertib, Myd88, inhibit, IL-1R, IL-1R associated kinase, Interleukin-1 receptor associated kinase, IRAK, IRAK4, inflammation, lymphoma, rheumatoid, Toll

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Key Properties

No computed properties available.

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Protocol Information

CA-4948 (orb1298434)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 70.00
2 mg
$ 90.00
5 mg
$ 110.00
1 ml x 10 mM (in DMSO)
$ 120.00
10 mg
$ 130.00
25 mg
$ 220.00
50 mg
$ 370.00
100 mg
$ 610.00
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