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Chemical Structure| 501437-28-1 Chemical Structure| 501437-28-1

Structure of BI-D1870
CAS No.: 501437-28-1

Chemical Structure| 501437-28-1

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BI-D1870 is an ATP-competitive, cell-permeable, and brain-penetrant inhibitor of RSK isoforms, with IC50 values of 31 nM, 24 nM, 18 nM, and 15 nM for RSK1, RSK2, RSK3, and RSK4, respectively.

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Product Details of BI-D1870

CAS No. :501437-28-1
Formula : C19H23F2N5O2
M.W : 391.42
SMILES Code : O=C1N(C)C2=CN=C(NC3=CC(F)=C(O)C(F)=C3)N=C2N(CCC(C)C)C1C
MDL No. :MFCD11223662
InChI Key :DTEKTGDVSARYDS-UHFFFAOYSA-N
Pubchem ID :25023738

Safety of BI-D1870

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of BI-D1870

MAPK
PI3K-AKT

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
OCI-AML2 1 µM 72 hours Reduced cell proliferation and colony forming potential PMC10400424
MOLM-13 2 µM 72 hours Reduced cell proliferation and colony forming potential PMC10400424
HL-60 2 µM 72 hours Reduced cell proliferation and colony forming potential PMC10400424
Caco-2 cells 10 μM 24 hours BI-D1870 inhibits RSK phosphorylation, restores Caspase-8 activation, and thereby reverses SopF-mediated PANoptosis inhibition PMC9980482
NCM460 cells 10 μM 24 hours BI-D1870 inhibits RSK phosphorylation, restores Caspase-8 activation, and thereby reverses SopF-mediated PANoptosis inhibition PMC9980482
HCT116 colon carcinoma cells 10 µM 24 hours BI-D1870 induces p21 accumulation and protects cells from γ-irradiation-induced apoptosis, driving them into senescence PMC3920941
MCF-7/casp3 breast carcinoma cells 10 µM 24 hours BI-D1870 induces p21 expression and leads to cellular senescence PMC3920941
PaTu-8988t cells 5 μM 24 hours To assess the synergistic effect of RSK3 inhibition with EGFR inhibitor erlotinib by measuring apoptosis through PARP cleavage PMC3884526
BxPC-3 cells 1 μM 48 hours To evaluate the synergistic effect of RSK3 inhibition with erlotinib by measuring cell viability using MTT assays PMC3884526
rat primary vascular smooth muscle cells 1, 2, 5, 10 µM 24 hours inhibits PDGF-BB-induced cell proliferation PMC10179136
rat primary vascular smooth muscle cells 2, 5 µM 24 hours inhibits PDGF-BB-induced cell migration PMC10179136
YUMAC 5 μM 72 hours BI-D1870 as a single agent significantly inhibited the proliferation of YUMAC and YURIF cells. PMC6342201
YURIF 5 μM 72 hours BI-D1870 as a single agent significantly inhibited the proliferation of YUMAC and YURIF cells. PMC6342201
YUMACdr 5 μM 72 hours BI-D1870 as a single agent or in combination with vemurafenib and selumetinib significantly inhibited the proliferation of YUMACdr and YURIFdr dual-resistant cells. PMC6342201
YURIFdr 5 μM 72 hours BI-D1870 as a single agent or in combination with vemurafenib and selumetinib significantly inhibited the proliferation of YUMACdr and YURIFdr dual-resistant cells. PMC6342201
NCI-H929 4.00 μM 48 hours BI-D1870 showed a dose-dependent growth inhibitory effect on NCI-H929 cells with an IC50 of 4.00 μM. PMC8949999
OPM-2 4.34 μM 48 hours BI-D1870 showed a dose-dependent growth inhibitory effect on OPM-2 cells with an IC50 of 4.34 μM. PMC8949999
KMS-12-BM 3.88 μM 48 hours BI-D1870 showed a dose-dependent growth inhibitory effect on KMS-12-BM cells with an IC50 of 3.88 μM. PMC8949999
KMS-28-PE 4.95 μM 48 hours BI-D1870 showed a dose-dependent growth inhibitory effect on KMS-28-PE cells with an IC50 of 4.95 μM. PMC8949999
AMO-1 3.14 μM 48 hours BI-D1870 showed a dose-dependent growth inhibitory effect on AMO-1 cells with an IC50 of 3.14 μM. PMC8949999
RPMI8226 4.09 μM 48 hours BI-D1870 showed a dose-dependent growth inhibitory effect on RPMI8226 cells with an IC50 of 4.09 μM. PMC8949999

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.26mL

12.77mL

2.55mL

1.28mL

25.55mL

5.11mL

2.55mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2
 

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