cRY9M acetate
Based on 1 Customer Validation
cRY9M acetate is a cyclic peptide that binds to FGFR1, with a KD value of 58 nM. cRY9M acetate binds specifically to FGFR1, exhibits enhanced in vivo stability, and shows extremely low degradation in blood, urine and liver homogenate after injection. cRY9M acetate displays significant specific uptake in FGFR1-positive tumor xenograft models, while its uptake decreases in FGFR1-negative tumor models and blocking models. The NOTA-chelated precursor of cRY9M acetate can be labeled with 68Ga to obtain [68Ga]Ga-NOTA-cRY9M, which is used for research on non-invasive imaging of FGFR1 expression in non-small cell lung cancer.
For research use only. We do not sell to patients.
- Purity : 98.51%
- Formula: C59H89N23O12·xC2H4O2
- Molecular Weight:1312.48 (free base)
-
Storage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
All Radionuclide-Drug Conjugates (RDCs) Isoforms
More
Biological Activity
Description
In Vitro
[68Ga]Ga-NOTA-cRY9M (4 h) retains a radiochemical purity of over 95% after incubation in fetal bovine serum (FBS) at 37 °C for 4 hours[1].
[68Ga]Ga-NOTA-cRY9M (74 kBq; 15-120 min) exhibits time-dependent and FGFR1-specific cellular uptake in Calu-3, NCI-H520 and NCI-H2170 cells[1].
[68Ga]Ga-NOTA-cRY9M (74 kBq; 2 h) inhibits the binding of FGFR1 to Calu-3 cells, with an IC50 of 62 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
[68Ga]Ga-NOTA-cRY9M (3.7 MBq; intravenous injection; single dose) targets NSCLC xenografts with moderate FGFR1 expression, reaching a peak tumor uptake of 3.11 %ID/g and a maximum tumor-to-muscle ratio of 4.10[1].
[68Ga]Ga-NOTA-cRY9M (3.7 MBq; intravenous injection; single dose) shows extremely low uptake in FGFR1-low-expressing NSCLC xenografts, with a maximum tumor uptake rate of 1.20 %ID/g and a low tumor-to-muscle ratio[1].
Pretreatment with NOTA-cRY9M (intravenous injection; single dose, 30 minutes in advance, 200-fold excess) blocks the FGFR1-specific uptake of [68Ga]Ga-NOTA-cRY9M (3.7 MBq; intravenous injection; single dose) in Calu-3 xenograft tumors, reducing the maximum tumor uptake to 1.45 %ID/g[1].
[68Ga]Ga-NOTA-cRY9M (3.7 MBq; intravenous injection; single administration) can specifically target NSCLC PDX tumors with high FGFR1 expression, reaching a peak tumor uptake of 3.84 %ID/g and a maximum tumor-to-muscle ratio of 5.28; pre-administration of an excess unlabeled peptide (200-fold excess; intravenous injection; single administration, 30 minutes in advance) blocks its uptake[1].
Uptake of [68Ga]Ga-NOTA-cRY9M (3.7 MBq; intravenous injection; single administration) in NSCLC PDX tumors correlates with FGFR1 expression, showing moderate accumulation in PDX-M tumors[1].
[68Ga]Ga-NOTA-cRY9M (3.7 MBq; intravenous injection; single dose) shows extremely low uptake in FGFR1-low-expressing NSCLC PDX tumors, which is consistent with the low target expression[1].
[68Ga]Ga-NOTA-cRY9M (3.7 MBq; intravenous injection; single dose) can specifically target FGFR1-positive breast cancer xenografts, and its uptake level correlates with target expression[1].
[68Ga]Ga-NOTA-cRY9M (3.7 MBq; intravenous injection; single administration) specifically targets FGFR1-positive pancreatic cancer xenografts, with its accumulation level correlated with target expression[1].
[68Ga]Ga-NOTA-cRY9M (3.7 MBq; intravenous injection; single dose) shows extremely low uptake in FGFR1-low-expressing breast cancer xenografts, which is consistent with the low expression level of the target[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c nude mice (male, 4 to 5 weeks old, 18−21 g, subcutaneous inoculation of 5 million Calu-3 cells mixed with 50% Corning Matrigel, tumors grown to 200−300 mm3 over 1−2 weeks)[1]
-
Dosage:3.7 MBq [68Ga]Ga-NOTA-cRY9M
-
Administration:i.v.; single dose
-
Result:Achieved peak tumor uptake of 3.69 %ID/g at 10 minutes postinjection, with gradual decline to 3.33 %ID/g by 60 minutes.
Exhibited primarily renal excretion with low hepatic retention.
Reached a maximum tumor-to-muscle ratio of 5.56 at 60 minutes, with tumor-to-liver and tumor-to-lung ratios of approximately 2.3 and 3.3, respectively, at 60 minutes.
-
Animal Model:BALB/c nude mice (male, 4 to 5 weeks old, 18−21 g, subcutaneous inoculation of 5 million NCI-H520 cells mixed with 50% Corning Matrigel, tumors grown to 200−300 mm3 over 1−2 weeks)[1]
-
Dosage:3.7 MBq [68Ga]Ga-NOTA-cRY9M
-
Administration:i.v.; single dose
-
Result:Achieved peak tumor uptake of 3.11 %ID/g at 10 minutes postinjection, with subsequent decline.
Reached a maximum tumor-to-muscle ratio of 4.10 at 60 minutes.
Showed tumor uptake of 2.61 %ID/g at 60 minutes postinjection via ex vivo biodistribution.
-
Animal Model:BALB/c nude mice (male, 4 to 5 weeks old, 18−21 g, subcutaneous inoculation of 5 million NCI-H2170 cells mixed with 50% Corning Matrigel, tumors grown to 200−300 mm3 over 1−2 weeks)[1]
-
Dosage:3.7 MBq [68Ga]Ga-NOTA-cRY9M
-
Administration:i.v.; single dose
-
Result:Reached a maximum tumor uptake of 1.20 %ID/g.
Maintained a consistently low tumor-to-muscle ratio of ~1.42 throughout the imaging window.
Showed tumor uptake of 0.91 %ID/g at 60 minutes postinjection via ex vivo biodistribution.
-
Animal Model:BALB/c nude mice (male, 4 to 5 weeks old, 18−21 g, subcutaneous inoculation of 5 million Calu-3 cells mixed with 50% Corning Matrigel, tumors grown to 200−300 mm3 over 1−2 weeks, blocking study with unlabeled NOTA-cRY9M)[1]
-
Dosage:3.7 MBq [68Ga]Ga-NOTA-cRY9M; 200-fold excess unlabeled NOTA-cRY9M
-
Administration:i.v.; single dose (tracer); i.v.; single dose (unlabeled peptide, 30 minutes prior to tracer)
-
Result:Reduced maximal tumor accumulation to 1.45 %ID/g at 60 minutes postinjection.
Reached a tumor-to-muscle ratio of only 1.77 at 60 minutes.
-
Animal Model:BALB/c nude mice (male, 4 to 5 weeks old, 18−21 g, patient-derived xenograft model PDX-H, established via subcutaneous implantation of 3 mm3 NSCLC patient tumor tissue into secondary BALB/c nude mice, tumors grown to appropriate size)[1]
-
Dosage:3.7 MBq [68Ga]Ga-NOTA-cRY9M; 200-fold excess unlabeled NOTA-cRY9M (blocking study)
-
Administration:i.v.; single dose (tracer); i.v.; single dose (unlabeled peptide, 30 minutes prior to tracer, blocking study)
-
Result:Achieved peak tumor uptake of 3.84 %ID/g at 10 minutes postinjection.
Reached a maximum tumor-to-muscle ratio of 5.28.
Reduced tumor uptake to 1.28 %ID/g after pretreatment with unlabeled NOTA-cRY9M.
-
Animal Model:BALB/c nude mice (male, 4 to 5 weeks old, 18−21 g, patient-derived xenograft model PDX-M, established via subcutaneous implantation of 3 mm3 NSCLC patient tumor tissue into secondary BALB/c nude mice, tumors grown to appropriate size)[1]
-
Dosage:3.7 MBq [68Ga]Ga-NOTA-cRY9M
-
Administration:i.v.; single dose
-
Result:Exhibited tumor uptake levels intermediate between PDX-H and PDX-L, with corresponding tumor-to-muscle ratios consistent with FGFR1 expression levels.
-
Animal Model:BALB/c nude mice (male, 4 to 5 weeks old, 18−21 g, patient-derived xenograft model PDX-L, established via subcutaneous implantation of 3 mm3 NSCLC patient tumor tissue into secondary BALB/c nude mice, tumors grown to appropriate size)[1]
-
Dosage:3.7 MBq [68Ga]Ga-NOTA-cRY9M
-
Administration:i.v.; single dose
-
Result:Exhibited minimal tumor uptake, comparable to background levels.
-
Animal Model:BALB/c nude mice (male, 4 to 5 weeks old, 18−21 g, subcutaneous inoculation of MDA-MB-231 cells mixed with 50% Corning Matrigel, tumors grown to appropriate size)[1]
-
Dosage:3.7 MBq [68Ga]Ga-NOTA-cRY9M
-
Administration:i.v.; single dose
-
Result:Showed significant accumulation in MDA-MB-231 tumors (FGFR1-positive), correlating with FGFR1 expression levels.
-
Animal Model:BALB/c nude mice (male, 4 to 5 weeks old, 18−21 g, subcutaneous inoculation of PANC-1 cells mixed with 50% Corning Matrigel, tumors grown to appropriate size)[1]
-
Dosage:3.7 MBq [68Ga]Ga-NOTA-cRY9M
-
Administration:i.v.; single dose
-
Result:Showed significant accumulation in PANC-1 tumors (FGFR1-positive), correlating with FGFR1 expression levels.
-
Animal Model:BALB/c nude mice (male, 4 to 5 weeks old, 18−21 g, subcutaneous inoculation of MDA-MB-468 cells mixed with 50% Corning Matrigel, tumors grown to appropriate size)[1]
-
Dosage:3.7 MBq [68Ga]Ga-NOTA-cRY9M
-
Administration:i.v.; single dose
-
Result:Showed minimal accumulation in MDA-MB-468 tumors (FGFR1-low), correlating with low target expression.
-
Animal Model:BALB/c nude mice (male, 4 to 5 weeks old, 18−21 g, subcutaneous inoculation of FGFR1-knockdown Calu-3 cells mixed with 50% Corning Matrigel, tumors grown to appropriate size)[1]
-
Dosage:3.7 MBq [68Ga]Ga-NOTA-cRY9M
-
Administration:i.v.; single dose
-
Result:Exhibited substantial reduction in tracer uptake (1.10 %ID/g) in FGFR1-knockdown Calu-3 xenografts compared to control Calu-3 tumors (3.83 %ID/g).
Showed correspondingly lower tumor-to-muscle ratios (2.11 vs 5.89) in FGFR1-knockdown vs control tumors.
Chemical Information
-
Appearance Solid
-
Molecular Weight 1312.48 (free base)
-
Formula C59H89N23O12·xC2H4O2
-
Color White to off-white
-
SMILES
O=C(N[C@@H](CC1=CNC2=CC=CC=C12)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CCCCN)C(N[C@@H](CCC(N)=O)C(N[C@@H]([C@H](O)C)C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC3=CNC=N3)C(N[C@H]4CC5=CC=C(C=C5)O)=O)=O)=O)=O)=O)=O)=O)[C@H](CCCNC(N)=N)NC4=O.CC(O)=O.[x]
-
Sequence
Cyclo(Arg-Trp-Arg-Lys-Gln-Thr-Arg-His-Tyr)
-
Sequence Shortening
Cyclo(RWRKQTRHY)
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
In Vitro:
DMSO : 100 mg/mL (Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL; Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
cRY9M acetate Related Classifications
HY-P11853A Related Classifications
Powered by Bioz