Fig. 1 · Structure

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SB 743921

Cat. No. A10828 CAS 940929-33-9

KSP Inhibitor

SB 743921, a second generation KSP inhibitor, is a highly potent and active therapeutic in preclinical models of cancer.

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Biological Activity

Target & Activity

Target Activity Value
KSP(MX1cells) IC50 0.06nM
KSP(Colo205cells) IC50 0.07nM
KSP ki 0.1nM
KSP(SKOV3cells) IC50 0.2nM
KSP(MV522cells) IC50 1.7nM
KSP(P388cells) IC50 14.4nM

6 targets · Scroll to view more

In Vitro Studies

Exposure to SB 743921 at 1 nmol/l and 5 nmol/l for 24 h significantly increased the G2/M phase in MDA-MB-231 cells compared with the DMSO control. The same treatment significantly increased the G2/M phase in MCF-7 cells compared with the DMSO control. In KMS20 cells, pretreatment with SB 743921 at 1 nM for the indicated times significantly reduced levels of SOD2, TFAM, Mcl-1, and cyclin D1 compared with control cells. [1,2]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

G2/M phase in MDA-MB-231 cells

Cell-based study · MDA-MB-231 [1]

MDA-MB-231 cells were exposed to SB 743921 at 1 nmol/l and 5 nmol/l for 24 h. The G2/M phase was significantly increased compared with the DMSO control.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
G2/M phaseReported result 1 and 5 nmol/l for 24 h: the G2/M phase was significantly increased compared with the DMSO control.[1]

Literature-Reported Treatment Conditions

Treatment concentration
1 nmol/l, and 5 nmol/l
Exposure duration
24 h
Method
exposed to SB743921
Vehicle
DMSO
Methods and source locations

Compound reported in the paper: SB 743921

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and methods > Cell lines and chemicals (S3); Materials and methods > Cell-cycle analysis (S19); Results > SB743921 induces cell-cycle arrest and apoptosis in breast cancer cells (S54, S55); Fig. 3 legend (S124)

G2/M phase: G2/M phase; comparator: DMSO control — Results > SB743921 induces cell-cycle arrest and apoptosis in breast cancer cells (S54, S55); Fig. 3 legend (S124)

Expression changes in KMS20 cells

Cell-based study · KMS20 cells [2]

KMS20 cells were pretreated with SB 743921 at 1 nM for the indicated times. Levels of SOD2, TFAM, Mcl-1, and cyclin D1 were significantly reduced compared with control cells.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Relative expression levels of SOD2, TFAM, Mcl-1, and cyclin D1Reported result 1 nM, for the indicated times: Levels of superoxide dismutase (SOD) 2; cyclin D1; TFAM; and an antiapoptotic Bcl-2 homologue, Mcl-1; were significantly reduced in SB743921-treated cells compared with control cells.[2]

Literature-Reported Treatment Conditions

Treatment concentration
1 nM
Exposure duration
the indicated times
Method
pretreated
Reported limits
Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: SB 743921

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

RESULTS > SB743921 potently induces cell death in multiple myeloma cells (S9); RESULTS > SB743921 induces cell death via inhibition of the NF-κB signaling pathway (S40); Fig. 3. legend (S91)

Relative expression levels of SOD2, TFAM, Mcl-1, and cyclin D1: Relative expression levels of SOD2, TFAM, Mcl-1, and cyclin D1; comparator: control cells — RESULTS > SB743921 potently induces cell death in multiple myeloma cells (S9); RESULTS > SB743921 induces cell death via inhibition of the NF-κB signaling pathway (S40); Fig. 3. legend (S91)

G2/M phase in MCF-7 cells

Cell-based study · MCF-7 [1]

MCF-7 cells were exposed to SB 743921 at 1 nmol/l and 5 nmol/l for 24 h. The G2/M phase was significantly increased compared with the DMSO control.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
G2/M phaseReported result 1 and 5 nmol/l for 24 h: the G2/M phase was significantly increased compared with the DMSO control.[1]

Literature-Reported Treatment Conditions

Treatment concentration
1 nmol/l, and 5 nmol/l
Exposure duration
24 h
Method
exposed to SB743921
Vehicle
DMSO
Methods and source locations

Compound reported in the paper: SB 743921

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Materials and methods > Cell lines and chemicals (S3); Materials and methods > Cell-cycle analysis (S19); Results > SB743921 induces cell-cycle arrest and apoptosis in breast cancer cells (S54, S55); Fig. 3 legend (S124)

G2/M phase: G2/M phase; comparator: DMSO control — Results > SB743921 induces cell-cycle arrest and apoptosis in breast cancer cells (S54, S55); Fig. 3 legend (S124)

In Vivo Studies

SB 743921 was administered intraperitoneally to female nude mice bearing SK-CHA-1 CDX models. Treatment significantly decreased tumor growth compared with saline treatment. [3]

Tumor growth in SK-CHA-1 CDX models

Animal study · SK-CHA-1 CDX models; nude mice; female, 6w; n = 6 [3]

Female nude mice bearing SK-CHA-1 CDX models received SB 743921 intraperitoneally. Treatment significantly decreased tumor growth compared with saline treatment.

Measured endpoints — not treatment concentrations
EndpointReported resultReference
Tumor volumes of SK-CHA-1 CDX modelsReported result treatment with SB743921 significantly decreased tumor growth, compared with saline treatment (p = 0.0198, after eight treatment injections, two-sided unpaired t test)[3]

Conditions shared by the study groups

Route
intraperitoneally
Treatment course
twice a week for six weeks
Study groups and reported outcomes
Group / doseComparatorObserved resultReference
SB 743921 5 mg/kgsaline (n = 6)treatment with SB743921 significantly decreased tumor growth, compared with saline treatment (p = 0.0198, after eight treatment injections, two-sided unpaired t test)[3]
SB 743921 5 mg/kg
Model: SK-CHA-1 CDX models; nude mice; female, 6w; n = 6
Reported limits: Not stated in the sentences used: vehicle.
Methods and source locations

Compound reported in the paper: SB 743921

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Results > Tumor suppression in CCA CDX models by KSP inhibition (S111, S113, S116, S117); Materials and methods > Xenograft tumor experiments (S244, S246)

Tumor volumes of SK-CHA-1 CDX models: Tumor volumes of SK-CHA-1 CDX models; comparator: saline (n = 6) — Results > Tumor suppression in CCA CDX models by KSP inhibition (S113, S116)

SB 743921 5 mg/kg · Results > Tumor suppression in CCA CDX models by KSP inhibition (S111, S113)

Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 940929-33-9
Applications KSP Inhibitor
Formula C31H33N2O3.HCl
Molecular Weight 553.5
SMILES
CC1=CC=C(C=C1)C(=O)N(CCCN)[C@@H](C2=C(C(=O)C3=C(O2)C=C(C=C3)Cl)CC4=CC=CC=C4)C(C)C.Cl

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 103 mg/mL (186.08 mM)
Water 20 mg/mL (36.13 mM)
Ethanol 103 mg/mL (186.08 mM)

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
28 mg/mL
Vehicle
Saline pH5.0

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

  1. [1] Zhu L, Xiao F, Yu Y, et al. KSP inhibitor SB743921 inhibits growth and induces apoptosis of breast cancer cells by regulating p53, Bcl-2, and DTL. Anticancer Drugs (2016). PMID: 27379929 DOI: 10.1097/CAD.0000000000000402 Source material
  2. [2] Song IS, Jeong YJ, Nyamaa B, et al. KSP inhibitor SB743921 induces death of multiple myeloma cells via inhibition of the NF-κB signaling pathway. BMB Rep (2015). PMID: 25772758 DOI: 10.5483/bmbrep.2015.48.10.015 Source material
  3. [3] Shi Y, Cui X, Jiang T, et al. The therapeutic effect of KSP inhibitors in preclinical models of cholangiocarcinoma. Cell Death Dis (2022). PMID: 36123339 DOI: 10.1038/s41419-022-05247-0 Source material

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