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Chemical Structure| 1092788-83-4 Chemical Structure| 1092788-83-4
Chemical Structure| 1092788-83-4

PP121

CAS No.: 1092788-83-4

PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2,Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibitsDNA-PK with IC50 of 60 nM.

Synonyms: PP121

4.5 *For Research Use Only !

Cat. No.: A986976 Purity: 98%

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Product Details of PP121

CAS No. :1092788-83-4
Formula : C17H17N7
M.W : 319.36
SMILES Code : NC1=C2C(N(C3CCCC3)N=C2C4=CN=C(NC=C5)C5=C4)=NC=N1
Synonyms :
PP121
MDL No. :MFCD12912434
InChI Key :NVRXTLZYXZNATH-UHFFFAOYSA-N
Pubchem ID :24905142

Safety of PP121

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302
Precautionary Statements:P280-P305+P351+P338

Related Pathways of PP121

RTK
PI3K-AKT

Isoform Comparison

Biological Activity

Target
  • mTOR

    mTOR, IC50:13 nM

  • DNA-PK

    DNA-PK, IC50:60 nM

  • PDGFR

    PDGFR, IC50:2 nM

  • Src

    Src, IC50:14 nM

  • Abl

    Abl, IC50:18 nM

In Vitro:

Cell Line
Concentration Treated Time Description Reference
K562 cells 0.080 to 20 µM 120 min PMC2880455
BaF3 cells 0.080 to 20 µM 120 min PP121 inhibited Bcr-Abl induced tyrosine phosphorylation in BaF3 cells. PMC2880455
NIH3T3 cells 2.5 µM 2 h PP121 blocked tyrosine phosphorylation induced by v-Src and restored actin stress fiber staining. PMC2880455
TT thyroid carcinoma cells 0.040 to 10 µM 2 h PP121 inhibited Ret autophosphorylation in cells at low nanomolar concentrations. PMC2880455
LN229 cells 0.040 to 10 µM PP121 inhibited the phosphorylation of Akt, p70S6K and S6 in these cells, but had no effect on the phosphorylation of Erk at concentrations up to 10 µM. PMC2880455
U87 cells 0.040 to 10 µM To assess the accumulation of penciclovir in transduced cells, results showed no accumulation of penciclovir in transduced cells PMC2880455
Human bronchial epithelial cells (16HBE) 3.16 µM, 10 µM, 56.23 µM 24 hours or 48 hours PP121 had no effect on the viability of 16HBE cells at low (3.16 µM) and medium (10 µM) concentrations, but inhibited cell viability at high concentration (56.23 µM) after 48 hours. PMC10629066
Mouse tracheal rings (mTRs) 4.19 ± 0.06 µM (IC50), 14.98 ± 0.06 µM (IC75) PP121 relaxed precontracted mouse tracheal rings by blocking certain ion channels, including L-type voltage-dependent Ca2+ channels (L-VDCCs), nonselective cation channels (NSCCs), transient receptor potential channels (TRPCs), Na+/Ca2+ exchangers (NCXs) and K+ channels, and accelerating calcium mobilization. PMC10629066
Tyk-nu-GFP 1, 2, 5, 10 μM 72 hours Inhibited ovarian cancer cell proliferation PMC6946883
HeyA8-GFP 0.36–46 μM 16 hours Inhibited ovarian cancer cell adhesion and invasion PMC6946883
SKOV3ip1-GFP 0.36–46 μM 16 hours Inhibited ovarian cancer cell adhesion and invasion PMC6946883
Non-small cell lung cancer cells (NCI-H2170) 500 nM-10 µM 48 hours To evaluate the inhibitory effect of PP121 on the proliferation of non-small cell lung cancer cells, results showed that PP121 decreased cell viability in a dose-dependent manner. PMC10011948
Non-small cell lung cancer cells (NCI-H1975) 500 nM-10 µM 48 hours To evaluate the inhibitory effect of PP121 on the proliferation of non-small cell lung cancer cells, results showed that PP121 decreased cell viability in a dose-dependent manner. PMC10011948

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description Reference
BALB/c mice OVA-induced asthma mouse model Gavage 20 mg/kg or 50 mg/kg Once daily from Day 21 to Day 34 PP121 relieved airway hyperresponsiveness, systematic inflammation and mucus secretion in asthmatic mice via downregulation of inflammatory factors, mucins and the MAPK/Akt signaling pathway. PMC10629066
C57BL/6NCrl mice ID8p53−/− ovarian cancer model Intraperitoneal injection 5 μM Single injection followed by 16 hours Inhibited ovarian cancer cell adhesion and invasion PMC6946883

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.13mL

0.63mL

0.31mL

15.66mL

3.13mL

1.57mL

31.31mL

6.26mL

3.13mL

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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