CA-4948

Name: CA-4948
Brand: Selleck Chemicals
SKU: S8562
Rating: 5 (0 reviews)

For research use only.

Catalog No.S8562

CAS No. 1801343-74-7

CA-4948 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades, and demonstrates pharmacodynamic and antitumor activity in in vitro and in vivo nonclinical models. CA-4948 also inhibits FLT3.

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Biological Activity

Description

CA-4948 is a reversible kinase inhibitor that modulates IRAK4 function in both the toll-like receptor (TLR) and interleukin 1 receptor (IL-1R) signaling cascades, and demonstrates pharmacodynamic and antitumor activity in in vitro and in vivo nonclinical models. CA-4948 also inhibits FLT3.

Targets

TLR ^[1]
()

IL-1R ^[1]
()

IRAK4 ^[1]
()

FLT3 ^[1]
()

In vitro

In vitro, CA-4948 blocked downstream NF-κB pathway signaling, including secretion of proinflammatory cytokines, in Toll-like receptor stimulated THP1 leukemic cells^[2].

In vivo

CA-4948 exhibits favorable DMPK properties, oral bioavailability, and is well tolerated in mice. Furthermore, CA-4948 was previously shown to exhibit dose-dependent efficacy in ABC-DLBCL MYD88-L265P xenograft tumor models using cell lines OCI-LY3 and OCI-Ly10 and patient-derived tumors^[1]. drug treatment led to decreased viability of MDS/AML stem cells (CD34+/CD38-/Lin-ve) in vivo studies using a THP1 leukemia xenograft model in NSG mice^[2].

Protocol

Animal Research: ^[1]	- Collapse Animal Models: SCID Beige mice Dosages: 50 mg/kg Administration: p.o. (Only for Reference)

References

Solubility (25°C)

In vitro	DMSO	30 mg/mL (71.87 mM)
	Water	Insoluble
	Ethanol	Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information Download CA-4948 SDF

Molecular Weight	417.42
Formula	C₂₁H₁₉N₇O₃
CAS No.	1801343-74-7
Storage	3 years-20°C powder 2 years-80°C in solvent
Synonyms	N/A
Smiles	C1COCCN1C2=NC3=C(O2)C=C(C=N3)NC(=O)C4=CC=CC(=N4)C5=CN=C(C=C5)N

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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL， Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH₂O，mix and clarify.

Note：1.Please make sure the liquid is clear before adding the next solvent.
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Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2020-09-01)

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT04278768	Recruiting	Drug: CA-4948	Acute Myelogenous Leukemia\|Myelodysplastic Syndrome	Curis Inc.	July 6 2020	Phase 1
NCT03328078	Recruiting	Drug: CA-4948\|Drug: ibrutinib	Relapsed Hematologic Malignancy\|Refractory Hematologic Malignancy	Curis Inc.	December 28 2017	Phase 1

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