1. GPCR/G Protein
  2. Bombesin Receptor
  3. BIM-26226

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.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

BIM-26226

BIM-26226 Chemical Structure

CAS No. : 136207-23-3

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Based on 1 publication(s) in Google Scholar

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Description

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[1][2][3][4].

IC50 & Target

bombesin receptor[1]

In Vitro

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.

In Vivo

BIM-26226 (30 and 100 μg/kg, s.c., 3 times daily for 14 consecutive days) inhibits the GRP-stimulated growth of a pancreatic cancer transplanted in the rat but, alone, has little influence on tumor growth [1].
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.

Animal Model: Azaserine (HY-B0919)-induced pancreatic acinar carcinoma model established in Lewis rats[1]
Dosage: 30 and 100 μg/kg
Administration: Subcutaneous injection (s.c.), 3 times daily for 14 consecutive days
Result: Reduced the contents of protein, RNA, amylase and trypsin.
Did not significantly affect pancreatic growth parameters.
Animal Model: Colon cancer model induced by DHD/K12 tumor cell line established in male BDIX rats (12 weeks old) [3]
Dosage: 100 μg/kg
Administration: Subcutaneous injection (s.c.), once daily for 6 weeks
Result: Significantly decreased gastrinemia.
Had no effect on bombesin binding sites kDs and affinity site number Bmax.
Molecular Weight

1075.09

Formula

C49H63F5N12O10

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

{D-F5 Phe}-Gln-Trp-{D-Ala}-Val-Ala-His-Leu-OMe

Sequence Shortening

{D-F5 Phe}-QW-{D-Ala}-VAHL-OMe

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 (93.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9302 mL 4.6508 mL 9.3015 mL
5 mM 0.1860 mL 0.9302 mL 1.8603 mL
View the 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.

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Purity & Documentation
References

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
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
BIM-26226
Cat. No.:
HY-P0039
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