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BMS-911543

SKU: orb1300463

Description

BMS-911543 is a highly selective JAK2 inhibitor (IC50 = 1.1 nM) with significant selectivity over JAK1, JAK3, and TYK2. It is a valuable research tool for investigating JAK2-dependent pathways in myeloproliferative neoplasms and hematological malignancies, as evidenced in both in vitro and in vivo preclinical studies.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

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BMS-911543

Key Properties

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CAS Number1271022-90-2
MW432.52
Purity99.98%
FormulaC23H28N8O
SMILESCCn1c(cc2c1nc(Nc1cc(C)n(C)n1)c1ncn(C)c21)C(=O)N(C1CC1)C1CC1
TargetHistone Methyltransferase,Tyrosine Kinases,JAK

Bioactivity

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Target IC50
JAK3:350nM|AK1:1.1 nM|TYK2:75nM
In Vivo
BMS-911543 suppresses the pSTAT5 levels (mediated by wild type JAK2) relative to vehicle control when stimulated with thrombopoetin (TPO) in a mouse pharmacodynamic model. The responses are dose dependent and results in nearly complete normalization of pSTAT5 levels for 18 h at the highest oral dose of 30 mg/kg. At an intermediate 10 mg/kg oral dose, ～65% reduction is observed up to 18 h, whereas at the 5 mg/kg dose, approximately 50% reduction in pSTAT5 for 8 h is achieved. Observed pSTAT5 reductions correlates with exposures of BMS-911543, with AUC0–8h values of 23, 41, and 109 μM·h, respectively, for dose levels of 5, 10, and 30 mg/kg. In addition, BMS-911543 demonstrates a potent and sustained (2 mg/kg up to 7 h) PD effect in blocking pSTAT5 formation in mice grafted with human SET-2 cells harboring JAK2-V617F mutation. The absolute oral bioavailability in solution is >50% in mice, rats, dogs, and monkeys. In addition, the absorption of BMS-911543 is not significantly impacted by particle dissolution (suspension formulation), with a relative bioavailability (vs solution) of ～60% in rats and ～100% in dogs.
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In Vitro
BMS-911543 shows potent antiproliferative activity in the SET-2 as well as BaF3-V617F engineered cell lines (both dependent upon JAK2 pathway), with IC50 values of 60 and 70 nM, respectively. The antiproliferative activity of BMS-911543 in SET-2 and BaF3-V617F cells correlates with similar activity on constitutively active pSTAT5 (IC50 80 and 65 nM, respectively). In contrast, non-JAK2-dependent cell lines (A549, MDA-MB-231, MiaPaCa-2) are significantly less sensitive to the inhibitor treatment. The excellent biochemical selectivity versus JAK1/3 translates to good cellular and functional selectivity in an IL-2 mediated T-cell proliferation assay (IC50 990 nM). Also, cell lines that rely on other JAK family members, including CTLL2 and parental BaF3 cells stimulated with IL-3, shows weak antiproliferative activity for BMS-911543 (IC50 2.9 and 3.5 μM, respectively).
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Storage & Handling

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Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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SET-2, Tyrosine Kinases, TyrosineKinases, TYK2, BMS 911543, BMS911543, BMS-911543, Inhibitor, HistoneMethyltransferase, Histone Methyltransferase, JAK3, Janus kinase, JAK2, JAK, JAK1, inhibit

Similar Products

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  • BMS-911543

    BMS-911543 [orb1226630]

    >98% (HPLC)

    1271022-90-2

    432.5

    C23H28N8O

    1 g, 500 mg, 200 mg, 100 mg, 50 mg, 5 mg, 10 mg, 2 mg, 25 mg
Quality Guarantee

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID
50922691 ↗

Key Properties

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No computed properties available.

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BMS-911543 (orb1300463)

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Available Sizes

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1 mg
¥ 1,300.00
1 ml x 10 mM (in DMSO)
¥ 2,080.00
5 mg
¥ 2,080.00
10 mg
¥ 3,120.00
25 mg
¥ 5,720.00
50 mg
¥ 8,320.00
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