MedKoo Cat#: 564382 | Name: SEL24-B489 HCl
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

SEL24-B489 is a potent, dual pan-PIM/FLT3 inhibitor. SEL24-B489 exhibited significantly broader on-target activity in AML cell lines and primary AML blasts than selective FLT3-ITD or PIM inhibitors. SEL24-B489 also demonstrated marked activity in cells bearing FLT3 tyrosine kinase domain (TKD) mutations that lead to FLT3 inhibitor resistance. Moreover, SEL24-B489 inhibited the growth of a broad panel of AML cell lines in xenograft models with a clear pharmacodynamic-pharmacokinetic relationship.

Chemical Structure

SEL24-B489 HCl
SEL24-B489 HCl
CAS#SEL24-B489 HCl

Theoretical Analysis

MedKoo Cat#: 564382

Name: SEL24-B489 HCl

CAS#: SEL24-B489 HCl

Chemical Formula: C15H19Br2ClN4O2

Exact Mass: 0.0000

Molecular Weight: 482.60

Elemental Analysis: C, 37.33; H, 3.97; Br, 33.11; Cl, 7.35; N, 11.61; O, 6.63

Price and Availability

Size Price Availability Quantity
5mg USD 850.00 2 Weeks
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Synonym
SEL24 Hydrochloride; SEL-24 HCl; SEL 24; SEL24-B489 HCl; SEL 24-B489; SEL-24-B489; SEL24B489 HCl; SEL 24B489; SEL-24B489;
IUPAC/Chemical Name
5,6-Dibromo-4-nitro-2-(piperidin-4-yl)-1-(propan-2-yl)-1H-1,3-benzodiazole hydrochloride
InChi Key
KQKOTVOYBRIGIT-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H18Br2N4O2.ClH/c1-8(2)20-11-7-10(16)12(17)14(21(22)23)13(11)19-15(20)9-3-5-18-6-4-9;/h7-9,18H,3-6H2,1-2H3;1H
SMILES Code
CC(N1C(C2CCNCC2)=NC3=C([N+]([O-])=O)C(Br)=C(Br)C=C31)C.[H]Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
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.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
SEL24-B489 induced RS cell apoptosis. In a cHL xenograft model, SEL24-B489 delayed tumor growth by 95.8% (P = .0002). Furthermore, SEL24-B489 decreased the expression of multiple molecules engaged in developing the immunosuppressive microenvironment, including galectin-1 and PD-L1/2. In coculture experiments, T cells incubated with SEL24-B489-treated RS cells exhibited higher expression of activation markers than T cells coincubated with control RS cells.

Preparing Stock Solutions

The following data is based on the product molecular weight 482.60 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Wu M, Li C, Zhu X. FLT3 inhibitors in acute myeloid leukemia. J Hematol Oncol. 2018 Dec 4;11(1):133. doi: 10.1186/s13045-018-0675-4. PMID: 30514344; PMCID: PMC6280371. 2: Czardybon W, Windak R, Gołas A, Gałęzowski M, Sabiniarz A, Dolata I, Salwińska M, Guzik P, Zawadzka M, Gabor-Worwa E, Winnik B, Żurawska M, Kolasińska E, Wincza E, Bugaj M, Danielewicz M, Majewska E, Mazan M, Dubin G, Noyszewska-Kania M, Jabłońska E, Szydłowski M, Sewastianik T, Puła B, Szumera- Ciećkiewicz A, Prochorec-Sobieszek M, Mądro E, Lech-Marańda E, Warzocha K, Tamburini J, Juszczyński P, Brzózka K. A novel, dual pan-PIM/FLT3 inhibitor SEL24 exhibits broad therapeutic potential in acute myeloid leukemia. Oncotarget. 2018 Mar 30;9(24):16917-16931. doi: 10.18632/oncotarget.24747. PMID: 29682194; PMCID: PMC5908295. 3: Białopiotrowicz E, Górniak P, Noyszewska-Kania M, Puła B, Makuch-Łasica H, Nowak G, Bluszcz A, Szydłowski M, Jabłonska E, Piechna K, Sewastianik T, Polak A, Lech-Marańda E, Budziszewska BK, Wasylecka-Juszczyńska M, Borg K, Warzocha K, Czardybon W, Gałęzowski M, Windak R, Brzózka K, Juszczyński P. Microenvironment- induced PIM kinases promote CXCR4-triggered mTOR pathway required for chronic lymphocytic leukaemia cell migration. J Cell Mol Med. 2018 Jul;22(7):3548-3559. doi: 10.1111/jcmm.13632. Epub 2018 Apr 17. PMID: 29665227; PMCID: PMC6010703. 4: Szydłowski M, Prochorec-Sobieszek M, Szumera-Ciećkiewicz A, Derezińska E, Hoser G, Wasilewska D, Szymańska-Giemza O, Jabłońska E, Białopiotrowicz E, Sewastianik T, Polak A, Czardybon W, Gałęzowski M, Windak R, Zaucha JM, Warzocha K, Brzózka K, Juszczyński P. Expression of PIM kinases in Reed-Sternberg cells fosters immune privilege and tumor cell survival in Hodgkin lymphoma. Blood. 2017 Sep 21;130(12):1418-1429. doi: 10.1182/blood-2017-01-760702. Epub 2017 Jul 11. PMID: 28698206.