BIM-26226
Based on 1 Customer Validation
BIM-26226 is a selective gastrin-releasing peptide receptor (GRPR) (IC50 = 6 nM) and bombesin receptor (BN receptor) antagonist. BIM-26226 antagonizes BN- or GRP-stimulated amylase release with IC50 values of 0.3 nM and 0.2 nM, respectively. BIM-26226 is specific for the GRP-preferring BN receptor subtype with no interference with GRP receptor system. BIM-26226 can induce the synthesis of somatostatin receptor but has no significant effect on tumor growth.
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- Purity: 98.73%
- CAS No.: 136207-23-3
- 화학식: C49H63F5N12O10
- 분자량:1075.09
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보관:
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]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
bombesin receptor[1]
BIM-26226 (0.1 nM-1 μM, 24 h) significantly decreased [3H]thymidine incorporation in primary cultured pancreatic tumour cells[1].
BIM-26226 is specific for the GRP-preferring BN receptor subtype and is not able to inhibit binding of radio-labeled CCK-33, gastrin-17 or VIP in AR4-2J cells[2].
BIM-26226 (0.1 μM) is able to block the bombesin-induced increase of Ca2+ but fails to block the growth-stimulatory effect of bombesin[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BIM-26226 (100 μg/kg, s.c., once daily for 6 weeks) induces the synthesis of somatostatin receptor but has no effect on tumor growth in colon cancer rat model[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Azaserine (HY-B0919)-induced pancreatic acinar carcinoma model established in Lewis rats[1]
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Dosage:30 and 100 μg/kg
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Administration:Subcutaneous injection (s.c.), 3 times daily for 14 consecutive days
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Result:Reduced the contents of protein, RNA, amylase and trypsin.
Did not significantly affect pancreatic growth parameters.
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Animal Model:Colon cancer model induced by DHD/K12 tumor cell line established in male BDIX rats (12 weeks old) [3]
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Dosage:100 μg/kg
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Administration:Subcutaneous injection (s.c.), once daily for 6 weeks
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Result:Significantly decreased gastrinemia.
Had no effect on bombesin binding sites kDs and affinity site number Bmax.
Chemical Information
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CAS No. 136207-23-3
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Appearance Solid
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분자량 1075.09
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화학식 C49H63F5N12O10
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Color White to off-white
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Sequence
{D-F5 Phe}-Gln-Trp-{D-Ala}-Val-Ala-His-Leu-OMe
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Sequence Shortening
{D-F5 Phe}-QW-{D-Ala}-VAHL-OMe
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선적
Room temperature in continental US; may vary elsewhere.
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보관
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)
용액&용해도
DMSO : 100 mg/mL (93.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Dietrich JB, et, al. Effects of BIM26226, a potent and specific bombesin receptor antagonist, on amylase release and binding of bombesin-like peptides to AR4-2J cells. Regul Pept. 1994 Oct 21;53(3):165-73. [Content Brief]
[2]. Damgé C, et, al. Effect of the gastrin-releasing peptide antagonist BIM 26226 and lanreotide on an acinar pancreatic carcinoma. Eur J Pharmacol. 1998 Apr 17;347(1):77-86. [Content Brief]
[3]. Gouyon B, et al. In-vivo effect of somatostatin analog, lanreotide, and/or grp antagonist, bim-26226, on the growth of colon-cancer peritoneal carcinomatosis in the rat. Int J Oncol. 1995 Nov;7(5):1167-73. [Content Brief]
[4]. Bold RJ, et al. Bombesin stimulates the in vitro growth of a human gastric cancer cell line. J Cell Physiol. 1994 Dec;161(3):519-25. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 0.9302 mL | 4.6508 mL | 9.3015 mL | 23.2539 mL |
| 5 mM | 0.1860 mL | 0.9302 mL | 1.8603 mL | 4.6508 mL | |
| 10 mM | 0.0930 mL | 0.4651 mL | 0.9302 mL | 2.3254 mL | |
| 15 mM | 0.0620 mL | 0.3101 mL | 0.6201 mL | 1.5503 mL | |
| 20 mM | 0.0465 mL | 0.2325 mL | 0.4651 mL | 1.1627 mL | |
| 25 mM | 0.0372 mL | 0.1860 mL | 0.3721 mL | 0.9302 mL | |
| 30 mM | 0.0310 mL | 0.1550 mL | 0.3101 mL | 0.7751 mL | |
| 40 mM | 0.0233 mL | 0.1163 mL | 0.2325 mL | 0.5813 mL | |
| 50 mM | 0.0186 mL | 0.0930 mL | 0.1860 mL | 0.4651 mL | |
| 60 mM | 0.0155 mL | 0.0775 mL | 0.1550 mL | 0.3876 mL | |
| 80 mM | 0.0116 mL | 0.0581 mL | 0.1163 mL | 0.2907 mL |
BIM-26226 Related Classifications
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