Bleomycin hydrochloride

Bleomycin hydrochloride is a DNA synthesis inhibitor. Bleomycin hydrochloride is a DNA damaging agent. Bleomycin hydrochloride is an antitumor antibiotic.

Product information

CAS Number: 67763-87-5

Molecular Weight: 1451.00

Formula: C55H84ClN17O21S3

Chemical Name: (3-{[2-(2-{2-[(2R,3R)-2-[(2R,3R,4S)-4-[(2S)-2-({6-amino-2-[(1S)-1-{[(2R)-2-amino-2-carbamoylethyl]amino}-2-carbamoylethyl]-5-methylpyrimidin-4-yl}formamido)-3-{[(2S,3R,4R,5R,6R)-3-{[(2R,3S,4S,5R,6R)-4-(carbamoyloxy)-3,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-3-hydrogenio-4,5-dihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy}-3-(1H-imidazol-4-yl)propanamido]-3-hydroxy-2-methylpentanamido]-3-hydroxybutanamido]ethyl}-1,3-thiazol-4-yl)-1,3-thiazol-4-yl]formamido}propyl)dimethylsulfanium chloride

Smiles: [Cl-].CC1C(=NC(=NC=1N)[C@H](CC(N)=O)NC[C@@H](N)C(N)=O)C(=O)N[C@@H](C(O[C@H]1O[C@H](CO)[C@H](O)[C@@H](O)[C@H]1O[C@H]1O[C@H](CO)[C@@H](O)[C@H](OC(N)=O)[C@@H]1O)C1=CNC=N1)C(=O)N[C@@H](C)[C@H](O)[C@@H](C)C(=O)N[C@H]([C@@H](C)O)C(=O)NCCC1=NC(=CS1)C1=NC(=CS1)C(=O)NCCC[S+](C)C

InChiKey: BODDZCXQPQPRES-PATWWPTKSA-N

InChi: InChI=1S/C55H83N17O21S3.ClH/c1-20-33(69-46(72-44(20)58)25(12-31(57)76)64-13-24(56)45(59)82)50(86)71-35(41(26-14-61-19-65-26)91-54-43(39(80)37(78)29(15-73)90-54)92-53-40(81)42(93-55(60)88)38(79)30(16-74)89-53)51(87)66-22(3)36(77)21(2)47(83)70-34(23(4)75)49(85)63-10-8-32-67-28(18-94-32)52-68-27(17-95-52)48(84)62-9-7-11-96(5)6;/h14,17-19,21-25,29-30,34-43,53-54,64,73-75,77-81H,7-13,15-16,56H2,1-6H3,(H13-,57,58,59,60,61,62,63,65,66,69,70,71,72,76,82,83,84,85,86,87,88);1H/t21-,22+,23-,24-,25+,29-,30-,34-,35+,36-,37+,38-,39-,40+,41?,42+,43-,53-,54-;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 50 mg/mL (34.46 mM; ultrasonic and warming and heat to 60°C). H2O : 100 mg/mL (68.92 mM; Need ultrasonic).

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Bleomycin hydrochloride is chosen as the best-studied micronucleus inducers in human lymphocytes with different mechanisms of genotoxicity. The most frequent Bleomycin-induced DNA lesions are single and double strand breaks and single apuinic/apyrimidinic sites. At the same time Bleomycin is true radiomimetic compound, resembling almost completely the genetic effect of ionizing radiation. The IC50 value of Bleomycin hydrochloride for UT-SCC-19A cell line is 4.0±1.3 nM. UT-SCC-12A and UT-SCC-12B are both more resistant to Bleomycin; IC50 values are 14.2±2.8 nM and 13.0±1.1 nM, respectively. Bleomycin hydrochloride (50, 100 μM; for 24, 48 h) induce pulmonary fibrosis in RLE-6TN cell (50 μM) and A549 cell (100 μM).

In Vivo:

Bleomycin hydrochloride treatment (3.5-4.0 mg/kg; intra-tracheal) on day 0, body weights decreases by day 4 then increases by Day 7 through the end of the study. Bleomycin hydrochloride (3.5-4.0 mg/kg; intra-tracheal) produces a statistically significant increase in lung hydroxyproline levels, and also increases right caudal lung lobe mass. Bleomycin hydrochloride (intratracheal instillation; 5.0 mg/kg/day) induces pulmonary fibrosis in eighty 8-week-old male BALB/c mice with weight about 20-30 g. Bleomycin induces the expression levels of α-SMA and collagen I. Bleomycin hydrochloride (intratracheally; 2.5 mg/kg; 1.25 mg/ml, approximately 50 µl per mouse) induces pulmonary fibrosis in male C57BL/6 mice (8 weeks old, average weight approximately 24.5 g).

References:

1. Hovhannisyan G, et al. Comparative analysis of individual chromosome involvement in micronuclei induced by bleomycin in human leukocytes. Mol Cytogenet. 2016 Jun 21;9:49.
2. Jaaskela-Saari HA, et al. Squamous cell cancer cell lines: sensitivity to bleomycin and suitability for animal xenograft studies. Acta Otolaryngol Suppl. 1997;529:241-4.
3. Corboz MR, et al. Therapeutic administration of inhaled INS1009, a LRX-15 prodrug formulation, inhibits bleomycin-induced pulmonary fibrosis in rats. Pulm Pharmacol Ther. 2018 Apr;49:95-103.
4. Ling Peng, et al. Scutellarin ameliorates pulmonary fibrosis through inhibiting NF-κB/NLRP3-mediated epithelial-mesenchymal transition and inflammation. Cell Death Dis. 2020 Nov 13;11(11):978.

Products are for research use only. Not for human use.