製品番号: HY-P11853

cRY9M

cRY9M is a cyclic peptide that binds to FGFR1, with a K_D value of 58 nM. cRY9M binds specifically to FGFR1, exhibits enhanced in vivo stability, and shows extremely low degradation in blood, urine and liver homogenate after injection. cRY9M 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 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.

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分子式: C₅₉H₈₉N₂₃O₁₂
分子量:1312.48

保管条件:

Please store the product under the recommended conditions in the Certificate of Analysis.

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製品説明

Radionuclide-Drug Conjugates (RDCs) アイソフォーム固有の製品をすべて表示 :

体外実験

[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.

体内実験

[⁶⁸Ga]Ga-NOTA-cRY9M (3.7 MBq; intravenous injection; single dose) exhibits superior tumor targeting in FGFR1-overexpressing NSCLC xenograft models, with a peak tumor uptake of 3.69 %ID/g and a maximum tumor-to-muscle ratio of 5.56^[1].
[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.

化学情報

分子量 1312.48
分子式 C₅₉H₈₉N₂₃O₁₂
配列

Cyclo(Arg-Trp-Arg-Lys-Gln-Thr-Arg-His-Tyr)
シーケンスの短縮

Cyclo(RWRKQTRHY)
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

Please store the product under the recommended conditions in the Certificate of Analysis.

純度とドキュメンテーション

取扱説明書 (2659 KB)

参考文献

[1]. Xue Y, et al. FGF2-Based Cyclic Peptide PET Tracer for Noninvasive Detection of FGFR1 Expression in Non-Small Cell Lung Cancer. Journal of medicinal chemistry. 2026 Feb 26;69(4):4755-4770. [Content Brief]

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cRY9M

Radionuclide-Drug Conjugates (RDCs) アイソフォーム固有の製品をすべて表示

生物活性

化学情報

純度とドキュメンテーション

参考文献

Calculators

Help & FAQs

cRY9M 関連分類

HY-P11853 関連分類