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Signaling Pathway

SGI-1776

HY-13287

(SGI 1776; SGI1776)

SGI-1776

SGI-1776 Chemical Structure

SGI-1776 is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM; 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin.

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Free sample   Apply now  
10 mM * 1 mL in DMSO $99 In-stock
5 mg $90 In-stock
10 mg $170 In-stock
50 mg $440 In-stock
100 mg Get quote
200 mg Get quote
Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €97 In-stock
5 mg €88 In-stock
10 mg €167 In-stock
50 mg €431 In-stock
100 mg Get quote
200 mg Get quote

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Product name: SGI-1776
Cat. No.: HY-13287

SGI-1776 Data Sheet

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    Purity: 98.82%

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    DataSheet

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    COA

Related Compound Libraries

Biological Activity of SGI-1776

SGI-1776 is a novel ATP competitive inhibitor of Pim1 with IC50 of 7 nM; 50- and 10-fold selective versus Pim2 and Pim3, also potent to Flt3 and haspin.
IC50 value: 7 nM [1]
Target: Pim1
in vitro: In addition to Pim, SGI-1776 also potently targets FLT3 (IC50 = 44nM). Treatment of AML cells with SGI-1776 results in a concentration-dependent induction of apoptosis. Importantly, SGI-1776 is also cytotoxic in AML primary cells, irrespective of FLT3 mutation status and results in Mcl-1 protein decline [1]. Treatment of CLL cells with SGI-1776 results in a concentration-dependent induction of apoptosis. SGI-1776 induces apoptosis in CLL and that the mechanism involves Mcl-1 reduction. Apoptosis induction coupled with the inhibition of RNA synthesis is observed in CLL cells treated with SGI-1776 [2]. SGI-1776 exhibites cytotoxic activity in vitro with a median relative IC50 of 3.1 mM. SGI-1776 induces tumor growth inhibition meeting criteria for intermediate EFS T/C activity in 1 of 39 evaluable models. In contrast, SGI-1776 induces complete responses of subcutaneous MV4;11 [3].
in vivo: Consistent with cell line data, xenograft model studies with mice bearing MV-4-11 tumors shows efficacy with SGI-1776. [1] SGI-1776 has shown preclinical activity against leukemia and solid tumor cell line models with IC50 values of 0.005–11.68 mM. SGI-1776 induces significant differences in EFS distribution in vivo in 9 of 31 solid tumor xenografts and in 1 of 8 of the evaluable ALL xenografts [3].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 405.42 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C20H22F3N5O
CAS No 1025065-69-3
Solvent & Solubility

DMSO ≥80mg/mL Water <1.2mg/mL Ethanol ≥80mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.4666 mL 12.3329 mL 24.6658 mL
5 mM 0.4933 mL 2.4666 mL 4.9332 mL
10 mM 0.2467 mL 1.2333 mL 2.4666 mL

References on SGI-1776

Inhibitor Kit

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