2. PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK Apoptosis
  3. PI3K Btk Apoptosis
  4. SRX3305

SRX3305 is an BTK/PI3K/BRD4 inhibitor with IC50s of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ, respectively. SRX3305 attenuates chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL) cell proliferation and promotes apoptosis in a dose-dependent fashion. SRX3305 yields potent anti-tumor effects but spares healthy bystander cells. SRX3305 inhibits the activation-induced proliferation of primary CLL cells in vitro and effectively blocks microenvironment-mediated survival signals. SRX3305 blocks CLL cell migration toward CXCL-12 and CXCL-13. SRX3305 maintains its anti-tumor effects in Ibrutinib (HY-10997)-resistant CLL cells. SRX3305 can be used for research in CLL, diffuse large B-cell lymphoma (DLBCL) and MCL.

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SRX3305

SRX3305 Chemical Structure

CAS No. : 2409965-28-0

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SRX3305 Related Antibodies

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Description

SRX3305 is an BTK/PI3K/BRD4 inhibitor with IC50s of 6.5 nM, 15 nM, and 4 nM toward BTK, PI3Kɑ and PI3Kδ, respectively. SRX3305 attenuates chronic lymphocytic leukemia (CLL) and mantle cell lymphoma (MCL) cell proliferation and promotes apoptosis in a dose-dependent fashion. SRX3305 yields potent anti-tumor effects but spares healthy bystander cells. SRX3305 inhibits the activation-induced proliferation of primary CLL cells in vitro and effectively blocks microenvironment-mediated survival signals. SRX3305 blocks CLL cell migration toward CXCL-12 and CXCL-13. SRX3305 maintains its anti-tumor effects in Ibrutinib (HY-10997)-resistant CLL cells. SRX3305 can be used for research in CLL, diffuse large B-cell lymphoma (DLBCL) and MCL[1][2].

IC50 & Target[2]

PI3Kα

15 nM (IC50)

PI3Kδ

4 nM (IC50)

In Vitro

SRX3305 (0.1-100 μM; 72 h) inhibits proliferation with an average IC50 of 1.38 µM across B-cell non-Hodgkin lymphoma (B-NHL) cell lines[1].
SRX3305 (0.1-100 μM; 72 h) reduces cell proliferation in DLBCL cells with IC50 values of ~290 nM in OCI-LY3 cells and ~920 nM in SU-DHL-6 cells[1].
SRX3305 (0.5-2 μM; 24-48 h) induces apoptosis in HG-3 and OSU-CLL cells in a dose-dependent manner[1].
SRX3305 (0.5-2 μM; 4 h) inhibits critical BCR survival signaling in OSU-CLL, MEC-1 and MEC-2 cell lines[1].
SRX3305 (0.16-5 μM; 48 h) inhibits primary malignant B-cell survival and proliferation in malignant B-cells isolated from Eμ-TCL1 (CLL model) and Eμ-Myc/TCL1 mice[1].
SRX3305 (0.5-2 μM; 48 h) disrupts stroma survival support and chemokine-induced migration in CLL[1].
SRX3305 (0.5-2 μM; 48 h) can overcome TME-induced survival signaling in MEC-1 cells[1].
SRX3305 (0.1-100 μM; 72 h) is active in ibrutinib-resistant HG-3 cells[1].
SRX3305 (10 nM-100 μM; 48 h) shows an IC50 of 1 nM in Mino cells, 58 nM in JeKo-1 cells, 1.1 μM in Granta cells, 1 μM in JeKo-1 BTK C481S mutant cells and 47 nM in Mino BTK C481S mutant cells[2].
SRX3305 (0.375-2 μM; 48 h) is minimally toxic to healthy donor peripheral blood mononuclear cells (PBMCs) or bystander healthy stromal cells and has low toxicity to healthy donor B-cells[2].
SRX3305 (0.1-10 μM; 48 h) has anti-tumor effect in primary Eμ-Myc tumor samples[2].
SRX3305 (0.01-0.5 μM; 1 h) blocks activation of both BTK and AKT[2].
SRX3305 (0.01-1 μM; 1 h) shows improved efficacy in MCL and Ibrutinib-resistant MCL cells[2].
SRX3305 (1 h) retains inhibition of BTK and AKT phosphorylation in Mino cells after inhibitor wash out experiments[2].
SRX3305 (0.5-2 μM; 24 h) inhibits JeKo-1 and Mino cells proliferation through inducing S/G2 phase cell cycle arrest and promoting apoptosis[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SRX3305 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: B-cell non-Hodgkin lymphoma cell lines
Concentration: 0.1 μM; 1 μM; 10 μM; 100 μM
Incubation Time: 72 h
Result: Significantly inhibited CLL cell proliferation in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: HG-3 and OSU-CLL cell lines
Concentration: 0.5 μM; 1 μM; 2 μM
Incubation Time: 24 h; 48 h
Result: Induced apoptosis in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: OSU-CLL, MEC-1 and MEC-2 cell lines
Concentration: 0.5 μM; 1 μM; 2 μM
Incubation Time: 4 h
Result: Effectively inhibited the phosphorylation of BTK and PRAS40 (indicative of PI3K/AKT signaling) and reduced MYC expression.

Western Blot Analysis[1]

Cell Line: OSU-CLL and MEC-1 cell lines
Concentration: 0.5 μM plus inhibitor treatment; 1 μM plus inhibitor treatment; 2 μM plus inhibitor treatment
Incubation Time: 4 h
Result: Decreased phosphorylation of BTK (p-BTK) and PRAS40 (p-PRAS40) and reduced MYC expression in continuous inhibitor treatment.
Retained the inhibition of p-BTK following treatment washout.
Marked inhibition of p-PRAS40 and MYC expression after treatment washout was maintained.

Cell Proliferation Assay[1]

Cell Line: patient-derived CLL cells
Concentration: 0.16 μM plus CpG (3.2 μM); 0.31 μM plus CpG (3.2 μM); 0.63 μM plus CpG (3.2 μM); 1.25 μM plus CpG (3.2 μM); 2.5 μM plus CpG (3.2 μM); 5 μM plus CpG (3.2 μM)
Incubation Time: 48 h
Result: Reversed CpG ODN-mediated proliferation reflected by reduced MYC levels in primary CLL cells.

Western Blot Analysis[1]

Cell Line: patient-derived CLL cells
Concentration: 0.5 μM plus CpG (3.2 μM); 1 μM plus CpG (3.2 μM); 2 μM plus CpG (3.2 μM)
Incubation Time: 48 h
Result: Induced the accumulation of P21 (cyclin-dependent kinase inhibitor), indicative of cell cycle arrest.
Did not influence the proliferation under unstimulated/basal conditions.

Cell Cytotoxicity Assay[1]

Cell Line: malignant B-cells isolated from Eμ-TCL1 (CLL model) and Eμ-Myc/TCL1 mice
Concentration: 0.5 μM; 1 μM; 2 μM
Incubation Time: 48 h
Result: Induced significant cytotoxicity in Eμ-TCL1 and Eμ-Myc/TCL1-derived malignant cells in a dose-dependent manner, suggesting promising therapeutic benefits in aggressive CLL and associated lymphomas.

Cell Viability Assay[1]

Cell Line: co-culture of primary CLL cells on BM-derived stromal cells
Concentration: 0.5 μM; 1 μM; 2 μM
Incubation Time: 48 h
Result: Reduced CLL cell viability in a dose-dependent manner despite stroma protection.
Did not have toxicity to the stromal cells, indicating that CLL cell cytotoxicity is not a function of reduced stroma viability.

Cell Migration Assay [1]

Cell Line: MEC-1 cells
Concentration: 0.5 μM; 1 μM; 2 μM
Incubation Time: 48 h
Result: Reduced the migration of MEC-1 cells towards CXCL-12 or CXCL-13.

Cell Proliferation Assay[1]

Cell Line: ibrutinib-resistant HG-3 cells
Concentration: 0.1 μM; 1 μM; 10 μM; 100 μM
Incubation Time: 72 h
Result: Remarkably decreased cell proliferation.

Western Blot Analysis[1]

Cell Line: ibrutinib-resistant HG-3 cells
Concentration: 1 μM; 2 μM
Incubation Time: 4 h
Result: Consistently decreased MYC expression and p-PRAS40 (PI3K target) and increased P21 levels in IR-HG3 cells.
Reduced BTK activation (phosphorylation).

Cell Viability Assay[2]

Cell Line: MCL cell lines JeKo-1, Mino, JeKo-1 BTK C481S and Mino BTK C481S
Concentration: 10 nM; 100 nM; 1 μM; 10 μM; 100 μM
Incubation Time: 48 h
Result: Exhibited strong anti-proliferative function.

Cell Viability Assay[2]

Cell Line: PBMCs
Concentration: 0.375 μM; 0.75 μM; 1.5 μM
Incubation Time: 48 h
Result: Had minimally toxicity.

Cell Viability Assay[2]

Cell Line: healthy donor B-cells
Concentration: 0.5 μM
Incubation Time: 48 h
Result: Exhibited low toxicity.

Cell Viability Assay[2]

Cell Line: bystander healthy stromal cells
Concentration: 0.5 μM; 1 μM; 2 μM
Incubation Time: 48 h
Result: Had minimally toxicity.

Cell Viability Assay[2]

Cell Line: primary Eμ-Myc tumor cells
Concentration: 0.1 μM; 0.3 μM; 1 μM; 3.2 μM; 10 μM
Incubation Time: 48 h
Result: Exhibited anti-tumor effect.

Western Blot Analysis[2]

Cell Line: IgM stimulated JeKo-1 and Mino cells
Concentration: 0.01 μM; 0.05 μM; 0.1 μM; 0.5 μM
Incubation Time: 1 h
Result: Decreased BTK phosphorylation at Tyr223 and AKT phosphorylation at Ser473.

Western Blot Analysis[2]

Cell Line: IgM-stimulated Granta cells
Concentration: 0.01 μM; 0.05 μM; 0.1 μM; 0.5 μM; 1 μM
Incubation Time: 1 h
Result: Showed dose dependent anti-proliferative activity.

Real Time qPCR[2]

Cell Line: JeKo-1 cells
Concentration: 0.5 μM
Incubation Time: 24 h
Result: Decreased the expression of cMYC.
Increased the expression of HEXIM1.

Apoptosis Analysis[2]

Cell Line: JeKo-1 and Mino cells
Concentration: 0.5 μM; 1 μM; 2 μM
Incubation Time: 24 h
Result: Induced apoptosis in JeKo-1 and Mino cells in a concentration-dependent manner.

Cell Cycle Analysis[2]

Cell Line: JeKo-1 and Mino cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Increased cell population in S phase and G2 phase.
Molecular Weight

424.47

Formula

C22H20N2O5S
CAS No.
SMILES

O=C1C=C(N2CCOCC2)OC3=C1SC=C3C4=CC5=C(OCCN5C(C=C)=O)C=C4
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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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SRX3305 Related Classifications

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Keywords:

SRX33052409965-28-0SRX 3305SRX-3305PI3KBtkApoptosisPhosphoinositide 3-kinaseBruton tyrosine kinaseBTK/PI3K/BRD4 inhibitorapoptosismicroenvironment-mediated survival signalsCXCL-12CXCL-13CLLDLBCLMCLInhibitorinhibitorinhibit

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