Busulfan (NSC-750)

For research use only.

Catalog No.S1692

9 publications

Busulfan (NSC-750) Chemical Structure

CAS No. 55-98-1

Busulfan (NSC-750) is a cell cycle non-specific alkylating antineoplastic agent. Busulfan induces apoptosis.

Selleck's Busulfan (NSC-750) has been cited by 9 publications

Purity & Quality Control

Choose Selective DNA alkylator Inhibitors

Biological Activity

Description Busulfan (NSC-750) is a cell cycle non-specific alkylating antineoplastic agent. Busulfan induces apoptosis.
In vitro

Busulfan inhibits the cobblestone area-forming cell frequency but fails to cause a significant increase in apoptosis in hematopoietic stem cell alike cells and progenitors. Busulfan inhibits the hematopoietic function of HSC alike cells and progenitors via an apoptosis-independent mechanism. Busulfan induces bone marrow hematopoietic cell senescence associated with an increased expression of p16Ink4a and p19Arf in a time-dependent manner. [1] Busulfan, an alkylating agent that causes DNA damage by cross-linking DNAs and DNA and proteins, induces senescence in normal human diploid WI38 fibroblasts through the extracellular signal-regulated kinase (Erk) and p38 mitogen-activated protein kinase (p38 MAPK) cascade independent of the p53-DNA damage pathway. Busulfan induces a transient reduction in GSH but a continuous increase in ROS production. [2] Busulfan-induced hypophosphorylation of Rb prevents apoptosis of spermatogonial stem cells by inhibiting PCNA expression in testicular cells. [3]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
SK-N-SH cells M4fwfXBzd2yrZnXyZZRqd25iYYPzZZk> MXOxNE0yODBizszN Mk[4O|IhcA>? NGK3PZNCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPLMW4uW0hiY3XscJMh[XRiMUCgeI8hOTByIIXNJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYm= Ml76QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR6MUS1N|IoRjJ2OEG0OVMzRC:jPh?=
SiMa cells M3TIR3Bzd2yrZnXyZZRqd25iYYPzZZk> NX71eXhkOTBvMUCwJO69VQ>? MVi3NkBp NHj3Zo1CdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIGPpUYEh[2WubIOgZZQhOTBidH:gNVAxKHWPIHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[Xl? M{XJT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEG0OVMzLz5{NEixOFU{OjxxYU6=
Kelly cells  M2rMRXBzd2yrZnXyZZRqd25iYYPzZZk> MWSxNE0yODBizszN Moq3O|IhcA>? NFXhSXBCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFvlcIx6KGOnbHzzJIF1KDFyIITvJFExOCC3TTDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7 NE\i[HY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEixOFU{Oid-MkS4NVQ2OzJ:L3G+
LS cells NFTlRmJRem:uaX\ldoF1cW:wIHHzd4F6 NV\rWoNmOTBvMUCwJO69VQ>? NIHSfI44OiCq MX7BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKEyVIHPlcIx{KGG2IEGwJJRwKDFyMDD1UUBi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5 M1;HfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OEG0OVMzLz5{NEixOFU{OjxxYU6=
K562 NGDkPWZCeG:ydH;zbZMh[XO|YYm= NFLXNW41QCCqcoO= MmDrTY5lfWO2aX;uJI9nKGGyb4D0c5NqeyCrbjDpcYF1cW6rYjDt[ZN6dGG2ZT3y[ZNqe3SjboSgbJVu[W5iS{W2NkBk\WyuczDh[pRmeiB2ODDodpM> MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQDN|OUS1OUc,OTh|M{m0OVU9N2F-
SK-N-MC MWPxTHRUKGG|c3H5 MXjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= M1q1flxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 M1rLNJFJXFNiYYPzZZk> MmHUdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6ELVXCZ|Eh[2WubIO= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
A673 MnjCdWhVWyCjc4PhfS=> NU\WOm1yeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhSTZ5MzDj[Yxteyl? M1mwc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
p-Y534 AR / AR ; 

PubMed: 27904688     


Western blotting probing influence of varied length (0 h, 12 h, 24 h and 48 h) of 60 mg/L busulfan treatment on AR protein expression level and AR phosphatization at Y534 site.

Ack1 / Src ; 

PubMed: 27904688     


Western blotting probing influence of 60 mg/L busulfan (at 48 h after treatment) on protein expression level of AR, Src and Ack 1 and AR phosphatization level at Y534 site.

27904688
Growth inhibition assay
Cell viability; 

PubMed: 24815002     


Percentage of viable cells (U2OS and MG-63) 24 h after different doses of busulfan. 

24815002
In vivo Busulfan-treated mice exhibit a marked increase in apoptosis and a decrease in testis weight. Busulfan is administered at the rate of 40 mg/kg body weight to induce a maximal number of apoptotic cells while minimizing the number of necrotic cells. [3] Busulfan conditioning and irradiation results in comparable sensitivity of HSC detection as evaluated by limiting dilution analysis in NOD/SCID mice. [4] Busulfan-transplanted mice has slow and incomplete lymphoid engraftment. Busulfan (20 mg/kg to 100 mg/kg) provides dose-dependent congenic lymphoid reconstitution in mice. [5]

Protocol

Solubility (25°C)

In vitro DMSO 49 mg/mL (198.94 mM)
Water Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+5% Tween 80+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 246.3
Formula

C6H14O6S2

Density 1.4 g/mL
CAS No. 55-98-1
Storage powder
in solvent
Synonyms N/A
Smiles CS(=O)(=O)OCCCCOS(=O)(=O)C

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04451200 Not yet recruiting Drug: Busulfan Injection Acute Leukemia|Mielodysplasic Syndrome|Myeloproliferative Neoplasm Institut Paoli-Calmettes November 2020 Phase 2
NCT03601286 Recruiting Drug: Lentiviral vector transduced CD34+ cells Severe Combined Immunodeficiency X-Linked Great Ormond Street Hospital for Children NHS Foundation Trust December 21 2018 Phase 1
NCT03235973 Unknown status Drug: Fludarabine-Cladribine-Busulfan conditioning regimen Leukemia Myeloid Acute|Leukemia Lymphoblastic Acute Institut Paoli-Calmettes April 28 2018 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    How can I reconstitute the drug for in vivo studies?

  • Answer:

    This compound also can be dissolved in 2% DMSO+30% PEG 300+5% Tween 80+ddH2O at 5mg/ml as a clear solution. When preparing the solution, please dissolve the compound in DMSO clearly first. Then add PEG and Tween. After they mixed well, dilute with water. S1692 in this formulation is not suitable for long-term storage. Please make the fresh solution each time before use.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID