Emavusertib
Emavusertib, also known as CA-4948 is a potent IRAK4/FLT3 inhibitor with anti-tumor activity. CA-4948 demonstrated good cellular activity in ABC DLBCL and AML cell lines. 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.
For research use only. We do not sell to patients.
Chemical Information
| Name | Emavusertib |
|---|---|
| Iupac Chemical Name | (R)-N-(5-(3-hydroxypyrrolidin-1-yl)-2-morpholinooxazolo[4,5-b]pyridin-6-yl)-2-(2-methylpyridin-4-yl)oxazole-4-carboxamide |
| Synonyms | CA-4948; CA 4948; CA4948; Emavusertib |
| Molecular Formula | C24H25N7O5 |
| Molecular Weight | 491.50 |
| Smile | O=C(C1=COC(C2=CC(C)=NC=C2)=N1)NC3=C(N4C[C@H](O)CC4)N=C5C(OC(N6CCOCC6)=N5)=C3 |
| InChiKey | SJHNWSAWWOAWJH-MRXNPFEDSA-N |
| InChi | InChI=1S/C24H25N7O5/c1-14-10-15(2-4-25-14)23-27-18(13-35-23)22(33)26-17-11-19-20(28-21(17)31-5-3-16(32)12-31)29-24(36-19)30-6-8-34-9-7-30/h2,4,10-11,13,16,32H,3,5-9,12H2,1H3,(H,26,33)/t16-/m1/s1 |
| CAS Number | 1801344-14-8 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white solid |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs. |
| HS Code |
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| Mechanism | |
| Cell study | |
| Animal study | |
| Clinical study |
1: Xu J, Qian Q, Xia M, Wang X, Wang H. Trichlorocarban induces developmental and immune toxicity to zebrafish (Danio rerio) by targeting TLR4/MyD88/NF-κB signaling pathway. Environ Pollut. 2021 Jan 10;273:116479. doi: 10.1016/j.envpol.2021.116479. Epub ahead of print. PMID: 33460871.
2: Gummadi VR, Boruah A, Ainan BR, Vare BR, Manda S, Gondle HP, Kumar SN, Mukherjee S, Gore ST, Krishnamurthy NR, Marappan S, Nayak SS, Nellore K, Balasubramanian WR, Bhumireddy A, Giri S, Gopinath S, Samiulla DS, Daginakatte G, Basavaraju A, Chelur S, Eswarappa R, Belliappa C, Subramanya HS, Booher RN, Ramachandra M, Samajdar S. Discovery of CA-4948, an Orally Bioavailable IRAK4 Inhibitor for Treatment of Hematologic Malignancies. ACS Med Chem Lett. 2020 Oct 14;11(12):2374-2381. doi: 10.1021/acsmedchemlett.0c00255. PMID: 33335659; PMCID: PMC7734642.
3: Wiese MD, Manning-Bennett AT, Abuhelwa AY. Investigational IRAK-4 inhibitors for the treatment of rheumatoid arthritis. Expert Opin Investig Drugs. 2020 May;29(5):475-482. doi: 10.1080/13543784.2020.1752660. Epub 2020 Apr 17. PMID: 32255710.
4: McElroy WT. Interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitors: an updated patent review (2016-2018). Expert Opin Ther Pat. 2019 Apr;29(4):243-259. doi: 10.1080/13543776.2019.1597850. Epub 2019 Mar 29. PMID: 30916602.
Chemical Structure
