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Chemical Structure| 1429617-90-2 Chemical Structure| 1429617-90-2

Structure of 7rh
CAS No.: 1429617-90-2

Chemical Structure| 1429617-90-2

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DDR1-IN-2 is an inhibitor of discoidin domain receptor 1 (DDR1) with IC50 of 13.1 nM, the IC50 of DDR2 is 203 nM.

Synonyms: DDR1-IN-2

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Product Details of 7rh

CAS No. :1429617-90-2
Formula : C30H29F3N6O
M.W : 546.59
SMILES Code : O=C(NC1=CC(C(F)(F)F)=CC(CN2CCN(C)CC2)=C1)C3=CC=C(CC)C(C#CC4=CN5C(N=C4)=CC=N5)=C3
Synonyms :
DDR1-IN-2
MDL No. :MFCD30185014
InChI Key :DDLPXZXBWGJRGK-UHFFFAOYSA-N
Pubchem ID :71550931

Safety of 7rh

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

Related Pathways of 7rh

RTK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
93T449 cells 0.00002-10 μM 5 days To evaluate the effect of 7RH on liposarcoma cell growth and proliferation, results showed that 7RH reduced cell growth and proliferation Clin Orthop Relat Res. 2023 Nov 1;481(11):2140-2153
SW 872 cells 0.00002-10 μM 5 days To evaluate the effect of 7RH on liposarcoma cell growth and proliferation, results showed that 7RH reduced cell growth and proliferation Clin Orthop Relat Res. 2023 Nov 1;481(11):2140-2153
MKN28 cells 0.18, 0.54, 1.62 μM Inhibited phosphorylation of DDR1 and PYK2, reduced colony formation and migration BMC Cancer. 2017 Jan 31;17(1):87
KATO-III cells 0.18, 0.54, 1.62 μM Inhibited phosphorylation of DDR1 and PYK2, reduced colony formation and migration BMC Cancer. 2017 Jan 31;17(1):87
KB cells 3μM 3 h Enhanced cytotoxicity of RG7787, IC50 reduced from >100 ng/ml to 6 ng/ml Cancer Res. 2016 Mar 15;76(6):1560-8
UM cells (92.1, Mel270) 10 μM 48 h To evaluate the effect of 7rh on ALDH activity in UM cells, results showed that 7rh significantly reduced the percentage of ALDH+ cells Signal Transduct Target Ther. 2021 May 12;6(1):176
UM cells (92.1, Mel270) 15 μM 24-48 h To evaluate the effect of 7rh on UM cell apoptosis, results showed that 7rh induced apoptosis in UM cells, as evidenced by PARP cleavage and caspase-3 activation Signal Transduct Target Ther. 2021 May 12;6(1):176
UM cells (92.1, Mel270, Omm1, Omm2.3) 0-20 μM 48 h To evaluate the effect of 7rh on UM cell proliferation, results showed that 7rh concentration-dependently inhibited UM cell growth with IC50 values ranging from 4 to 10 μM Signal Transduct Target Ther. 2021 May 12;6(1):176

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c-nu nude mice MKN28 xenograft model Oral 25 mg/kg Every 2 days for 15 days Suppressed tumor growth, reduced phosphorylation of DDR1 and PYK2 BMC Cancer. 2017 Jan 31;17(1):87
Nude mice Subcutaneous xenograft model in nude mice Intraperitoneal injection 8 mg/kg Once daily for 20 days To evaluate the inhibitory effect of 7RH on the growth of nasopharyngeal carcinoma tumors in vivo. The results showed that 7RH could significantly inhibit tumor growth Oncol Lett. 2016 Nov;12(5):3598-3608
Athymic nude mice A431/H9 and KLM1 xenograft models Oral gavage 10 or 20 mg/kg 7rh Daily for a total of 16 doses Combination of 7rh and RG7787 significantly enhanced antitumor activity, with 61% reduction in A431/H9 tumor volume and 89% reduction in KLM1 tumor volume Cancer Res. 2016 Mar 15;76(6):1560-8
BALB/c mice MSS CRC mouse model Oral 12.5 mg/kg Every three days, three times in total To evaluate the effect of 7rh in combination with PD-1 blockade NPJ Precis Oncol. 2024 Nov 7;8(1):253

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.83mL

0.37mL

0.18mL

9.15mL

1.83mL

0.91mL

18.30mL

3.66mL

1.83mL

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

References

 

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