Structure of AZD-7648
CAS No.: 2230820-11-6
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The BI-3802 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
AZD7648 is a highly potent and selective DNA-PK inhibitor with IC50 value of 92nM.
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Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
Batch number can be found on the product's label following the word 'Batch'.
Search for reports by entering the product batch number.
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CAS No. : | 2230820-11-6 |
Formula : | C18H20N8O2 |
M.W : | 380.40 |
SMILES Code : | O=C1N(C)C2=CN=C(NC3=CN4C(C=C3C)=NC=N4)N=C2N1C5CCOCC5 |
MDL No. : | MFCD32062688 |
InChI Key : | XISVSTPEXYIKJL-UHFFFAOYSA-N |
Pubchem ID : | 135151360 |
GHS Pictogram: |
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Signal Word: | Warning |
Hazard Statements: | H302-H315-H319-H335 |
Precautionary Statements: | P261-P305+P351+P338 |
In Vitro:
Cell Line
|
Concentration | Treated Time | Description | References |
HeLa cells | 1 mM | 1 hour | To study the binding mode of AZD-7648 with DNA-PKcs, revealing its mechanism of competitive inhibition of ATP binding | PMC8791830 |
A549 non-small cell lung cancer cells | 0.6 nM | 1 hour | Evaluate the inhibitory effect of AZD7648 on DNA-PKcs autophosphorylation | PMC6838110 |
OAW42 ovarian cancer cells | 3 μM | 16 hours | Evaluate the effect of AZD7648 in combination with doxorubicin on DNA damage and apoptosis | PMC6838110 |
HNSCC cell lines (FaDu, A253, Detroit 562, UMSCC12, UMSCC74A, UMSCC6) | 1 µM | 1-hour pretreatment | AZD-7648 significantly reduced clonogenic survival of HNSCC cell lines, particularly following X-ray and proton beam therapy. DER (dose enhancement ratio) ranged from 1.41–2.86 (X-rays) and 1.63–2.52 (proton beam). | PMC11169544 |
MC38 cells | 1 μM | 24 hours | To evaluate the radiosensitizing effect of AZD7648 on MC38 cells. Results showed that AZD7648 at 1 μmol/L significantly enhanced IR-induced cell death, with a DEF37 of 2.02. | PMC9401489 |
HSPCs (hematopoietic stem and progenitor cells) | 7 μM | 24 hours | Enhance HDR editing efficiency, reduce NHEJ, and increase the conversion rate of -175T>C and -158C>T in HSPCs | PMC11687217 |
Human airway basal stem cells (ABCs) | 0.5 μM | 24 hours | To evaluate the effect of AZD7648 on gene insertion efficiency, results showed AZD7648 significantly improved gene insertion efficiency (from 34.8% to 61.3%) | PMC11470261 |
UM-SCC-47 | 5 μM | 24 hours | Evaluate the radiosensitizing effect of AZD7648 on HPV+ HNSCC cells, showing significant increase in G2/M arrest and cell death. | PMC10887161 |
CAL33 | 5 μM | 24 hours | Evaluate the radiosensitizing effect of AZD7648 on HNSCC cells, showing significant inhibition of IR-induced DNA double-strand break repair and increased cell death. | PMC10887161 |
Cal78 | 1, 3, 10 µM | 24 hours | Pretreatment with AZD7648 significantly enhanced the inhibitory effect of X-ray and carbon ion irradiation on cell proliferation, leading to G2/M phase cell cycle arrest. | PMC11173223 |
SW-1353 | 1, 3, 10 µM | 24 hours | Pretreatment with AZD7648 significantly enhanced the inhibitory effect of X-ray and carbon ion irradiation on cell proliferation, leading to G2/M phase cell cycle arrest. | PMC11173223 |
HEL | 50-200 µM | 24-72 hours | To evaluate the effect of AZD-7648 on HEL cell density and viability. Results showed IC50 between 150-200 µM after 24 hours, decreasing to 97.7 µM and 85.5 µM after 48 and 72 hours, respectively. | PMC10607085 |
LAMA-84 | 100-200 µM | 24-72 hours | To evaluate the effect of AZD-7648 on LAMA-84 cell density and viability. Results showed IC50 values of 92.6 µM and 81.6 µM after 48 and 72 hours, respectively. | PMC10607085 |
K-562 | 10-200 µM | 24-72 hours | To evaluate the effect of AZD-7648 on K-562 cell density and viability. Results showed that IC50 was not reached (IC50 > 200 µM) within the tested concentration range. | PMC10607085 |
Primary human CD4+ T cells | 1 µM | 3 days | Evaluate the effect of AZD7648 on CRISPR/Cas9-mediated HDR-KI efficiency, results showed significant increase in HDR-KI efficiency | PMC10425386 |
HiPSC | 1 µM | 3 days | Evaluate the effect of AZD7648 on CRISPR/Cas9-mediated HDR-KI efficiency, results showed significant increase in HDR-KI efficiency | PMC10425386 |
HepG2 | 1 µM | 3 days | Evaluate the effect of AZD7648 on CRISPR/Cas9-mediated HDR-KI efficiency, results showed significant increase in HDR-KI efficiency | PMC10425386 |
Jurkat | 1 µM | 3 days | Evaluate the effect of AZD7648 on CRISPR/Cas9-mediated HDR-KI efficiency, results showed significant increase in HDR-KI efficiency | PMC10425386 |
HEK293T | 1 µM | 3 days | Evaluate the effect of AZD7648 on CRISPR/Cas9-mediated HDR-KI efficiency, results showed significant increase in HDR-KI efficiency | PMC10425386 |
Mature B-cell lines (3301015, 5680001) | 1-20 μM | 3 days | Evaluate AZD7648 effects on normal B-cell viability; results showed AZD7648 decreased viability of one or both B-cell lines at 1-20μM | PMC10111164 |
B-ALL cell lines (LAX56, BLQ5, LAX7R) | 1-20 μM | 3 days | Evaluate AZD7648 effects on B-ALL cell viability; results showed AZD7648 decreased viability at all tested concentrations | PMC10111164 |
MG63 cells | 10 µM | 48 hours | Evaluate the synergistic effect of AZD-7648 with DOX, results showed AZD-7648 significantly enhanced the inhibitory effect of DOX on osteosarcoma cells. | PMC11372366 |
U2OS cells | 10 µM | 48 hours | Evaluate the synergistic effect of AZD-7648 with DOX, results showed AZD-7648 significantly enhanced the inhibitory effect of DOX on osteosarcoma cells. | PMC11372366 |
HOS cells | 10 µM | 48 hours | Evaluate the synergistic effect of AZD-7648 with DOX, results showed AZD-7648 significantly enhanced the inhibitory effect of DOX on osteosarcoma cells. | PMC11372366 |
143B cells | 10 µM | 48 hours | Evaluate the synergistic effect of AZD-7648 with DOX, results showed AZD-7648 significantly enhanced the inhibitory effect of DOX on osteosarcoma cells. | PMC11372366 |
Primary human hematopoietic stem and progenitor cells (HSPCs) | 0.5 µM | 48 hours | Improving homology-directed repair (HDR) efficiency, achieving mean editing efficiency of 97% | PMC11147503 |
Healthy fibroblasts (SBLF8, SBLF9) | 5000 nM | 48 hours | AZD7648 alone had minimal toxicity to healthy fibroblasts, but combined with ionizing radiation reduced clonogenic survival | PMC11172136 |
HNSCC cell lines (Cal33) | 5000 nM | 48 hours | AZD7648 combined with ionizing radiation significantly increased cell death with supra-additive effects | PMC11172136 |
B2M gene-targeted CD34+ HSPCs | 0.33, 1, and 3 μM | 48 hours | To evaluate the effect of AZD7648 on NHEJ and HDR, results showed AZD7648 inhibited NHEJ and promoted HDR. | PMC11863497 |
CD34+ hematopoietic stem and progenitor cells (HSPCs) | 0.33, 1, and 3 μM | 48 hours | To evaluate the effect of AZD7648 on HDR efficiency, results showed AZD7648 significantly increased HDR efficiency. | PMC11863497 |
KG-1 | 100-200 µM | 48-72 hours | To evaluate the effect of AZD-7648 on KG-1 cell density and viability. Results showed IC50 of 159.9 µM after 72 hours. | PMC10607085 |
GOT1 | 1 μM | 5 days | To evaluate the effect of AZD7648 on PRRT-induced cell death, results showed that AZD7648 significantly increased PRRT-induced cell death. | PMC10283055 |
NCI-H69 | 1 μM | 7 days | To evaluate the effect of AZD7648 on the viability of PRRT-treated cells, results showed that AZD7648 significantly reduced the viability of PRRT-treated cells. | PMC10283055 |
BON1-SSTR2 | 1 μM | 7 days | To evaluate the effect of AZD7648 on the viability of PRRT-treated cells, results showed that AZD7648 significantly reduced the viability of PRRT-treated cells. | PMC10283055 |
EW8 cells | 0.1 μM | 72 hours | AZD-7648 synergized with etoposide, significantly reducing cell viability and proliferation | PMC11293986 |
TC-32 cells | 0.1 μM | 72 hours | AZD-7648 synergized with etoposide, significantly reducing cell viability and proliferation | PMC11293986 |
FaDu head and neck cancer cells | 0.6 μM | 72 hours | Evaluate the effect of AZD7648 in combination with olaparib on genomic instability and apoptosis in ATM-deficient cells | PMC6838110 |
VMCUB-1 | 0.01–20 μM | 72 hours | To evaluate the radiosensitizing effect of AZD7648 on bladder cancer cells, results showed a decrease in IC50 values with increasing radiation doses | PMC9220184 |
J82 | 0.01–20 μM | 72 hours | To evaluate the radiosensitizing effect of AZD7648 on bladder cancer cells, results showed a decrease in IC50 values with increasing radiation doses | PMC9220184 |
SCaBER | 0.01–20 μM | 72 hours | To evaluate the radiosensitizing effect of AZD7648 on bladder cancer cells, results showed a decrease in IC50 values with increasing radiation doses | PMC9220184 |
In Vivo:
Species
|
Animal Model
|
Administration | Dosage | Frequency | Description | References |
NBSGW mice | Immune-deficient mouse model | Transplant after in vitro treatment | 0.3 μM | 16 weeks | To evaluate the effect of AZD7648 on long-term engraftment of HDR-edited HSPCs, results showed AZD7648 significantly increased the long-term engraftment of HDR-edited cells. | PMC11863497 |
Nude mice | A549 xenograft model | Oral | 100 mg/kg | Once daily for 21 days | Evaluate the tumor growth inhibitory effect of AZD7648 in combination with radiotherapy | PMC6838110 |
Rj:NMRI-Foxn1nu/nu mice | BON1-SSTR2 and NCI-H69 xenograft models | Oral gavage | 50 mg/kg or 100 mg/kg | Once daily for 7 consecutive days | To evaluate the enhancement of PRRT anti-tumor effects by AZD7648, results showed that AZD7648 significantly enhanced the anti-tumor effects of PRRT. | PMC10283055 |
NBSGW mice | Β-thalassemia and sickle cell disease model | Tail vein injection | 7 μM | Single administration, observed for 16-18 weeks | Enhance HDR editing efficiency, reduce NHEJ, increase the conversion rate of -175T>C and -158C>T in HSPCs, and produce functional HbF in vivo | PMC11687217 |
BALB/c nude mice | Subcutaneous xenograft model | Oral | 70 mg/kg | Once daily for 14 days | Evaluate the synergistic effect of AZD-7648 with DOX, results showed the combination therapy significantly inhibited osteosarcoma growth. | PMC11372366 |
Mice | MC38, CT26, and B16-F10 syngeneic tumor models | Oral | 75 mg/kg | Once daily for 5 days | To evaluate the antitumor efficacy of AZD7648 in combination with RT. Results showed that the combination of AZD7648 and RT significantly improved tumor control, with complete tumor regressions observed in 75% and 42% of mice in MC38 and CT26 models, respectively. | PMC9401489 |
Nude mice | TC-32 and EW8 orthotopic xenograft models | AZD-7648 orally, etoposide intraperitoneally | AZD-7648 25 mg/kg BID, etoposide 10 mg/kg daily | Daily for 5 days, repeated every 2 weeks | Combination of AZD-7648 and etoposide led to tumor shrinkage, enhanced DNA damage and apoptosis | PMC11293986 |
Bio Calculators | ||||
Preparing Stock Solutions | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.63mL 0.53mL 0.26mL |
13.14mL 2.63mL 1.31mL |
26.29mL 5.26mL 2.63mL |
|
Dissolving Methods |
The prepared working fluid is recommended to be prepared now and used up as soon as possible in a short period of time. 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.
|
Tags: AZD-7648 | AZD7648 | AZD 7648 | DNA-PK | DNA-PK inhibitor | PI3K | Apoptosis | DNA-dependent protein kinase | Ataxia telangiectasia mutated | ATM and RAD3 related | Phosphoinositide 3-kinase | 2230820-11-6
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H320 | Causes eye irritation |
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H413 | May cause long-lasting harmful effects to aquatic life |
H420 | Harms public health and the environment by destroying ozone in the upper atmosphere |
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