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Chemical Structure| 860352-01-8 Chemical Structure| 860352-01-8

Structure of AZD-7762
CAS No.: 860352-01-8

Chemical Structure| 860352-01-8

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AZD-7762 is a potent ATP-competitive checkpoint kinase (Chk) inhibitor with an IC50 of 5 nM for Chk1.

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Product Details of AZD-7762

CAS No. :860352-01-8
Formula : C17H19FN4O2S
M.W : 362.42
SMILES Code : O=C(C1=C(NC(N)=O)C=C(C2=CC=CC(F)=C2)S1)N[C@@H]3CNCCC3
MDL No. :MFCD12406007
InChI Key :IAYGCINLNONXHY-LBPRGKRZSA-N
Pubchem ID :11152667

Safety of AZD-7762

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

Isoform Comparison

Biological Activity

Target
  • Chk1

    Chk1, IC50:5 nM

  • Chk2

    Chk2, IC50:<10 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Lkb1-null t2, t4, t5 cells 0-500 nM 4 days To evaluate the effect of AZD7762 alone or in combination with gemcitabine on the viability of Lkb1-null cells, the results showed that the combination significantly reduced cell viability. PMC5600859
HT29 cells 100 nM 6 h To test the efficacy of LMP-400 for inducing a substantial S-phase arrest and the extent to which this arrest could be abrogated by AZD7762, it was found that AZD7762 was able to reactivate DNA synthesis and re-establish a normal cell cycle profile. PMC3288175
HT29 cells 16, 31, 63, 125 nM 48 h To evaluate the potential impact of AZD7762 on LMP-400-induced cell killing, it was found that AZD7762 showed synergistic antiproliferative activity when combined with LMP-400 in HT29 cells. PMC3288175
UM-UC-3 20 nM 24 or 48 h To evaluate the effect of AZD7762 combined with gemcitabine on the viability of bladder cancer cells, the results showed that the combined use significantly reduced cell viability. PMC5209915
T24 10 nM 24 or 48 h To evaluate the effect of AZD7762 combined with gemcitabine on the viability of bladder cancer cells, the results showed that the combined use significantly reduced cell viability. PMC5209915
RT-112 10 nM 24 or 48 h To evaluate the effect of AZD7762 combined with gemcitabine on the viability of bladder cancer cells, the results showed that the combined use significantly reduced cell viability. PMC5209915
VM-CUB1 10 nM 24 or 48 h To evaluate the effect of AZD7762 combined with gemcitabine on the viability of bladder cancer cells, the results showed that the combined use significantly reduced cell viability. PMC5209915
MiaPaCa-2 cells 100 nM 24 h To evaluate the chemosensitization effect of AZD-7762 on pancreatic cancer cells, results showed that AZD-7762 significantly enhanced the cytotoxicity of gemcitabine when administered 24 h after gemcitabine treatment. PMC3107893
A549 100 nM 24 h AZD7762 partially reversed the A-macB-induced G2/M arrest and enhanced the cytotoxicity of A-macB. PMC5989808
H1299 100 nM 24 h AZD7762 partially reversed the A-macB-induced G2/M arrest and enhanced the cytotoxicity of A-macB. PMC5989808

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice NOD/SCID mice Intraperitoneal injection 25 mg/kg Every 24 and 42 hours The combination therapy of AZD7762 and irinotecan significantly inhibited tumor growth and prolonged survival in mice bearing TP53 mutant tumors PMC3314455
Mice Kras/p53/Lkb1 mice Intraperitoneal injection 25 mg/kg Once daily for two weeks To evaluate the effect of AZD7762 alone or in combination with gemcitabine on tumor volume in Kras/p53/Lkb1 mice, the results showed that the combination significantly reduced tumor volume and prolonged survival. PMC5600859
Nude mice Pancreatic cancer xenograft model Subcutaneous injection 25 mg/kg Once every 7 days for 14 days To evaluate the chemosensitization effect of AZD-7762 on pancreatic cancer xenograft models, results showed that AZD-7762 significantly inhibited tumor growth after gemcitabine treatment. PMC3107893
Mice MiaPaCa-2 xenograft model Subcutaneous injection 20mg/kg Administered on days 0, 1, 7, 8, 14, and 15 Evaluate the effect of AZD7762 in combination with gemcitabine and radiation on pancreatic cancer, showing significant tumor regression in the AZD7762+1Gy and GEM+1Gy groups PMC3048927

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.76mL

0.55mL

0.28mL

13.80mL

2.76mL

1.38mL

27.59mL

5.52mL

2.76mL

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