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ALX-270-379

Revised 04-Mar-05

Oxamflatin
SYNONYMS	(2E)-5-[3-(Phenylsulfonylamino)phenyl]pent-2-en-4-ynohydroxamic acid
PRODUCT LINE	Cancer
PRODUCT CATEGORY	Antitumor Agents (Apoptosis Inducers)

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-379-M001		1 mg	70.00 USD
ALX-270-379-M005		5 mg	275.00 USD

Product Specification

FORMULA:	C₁₇H₁₄N₂O₄S
MW:	342.4
PURITY:	≥95% (HPLC)
APPEARANCE:	Solid.
SOLUBILITY:	Soluble in DMSO, methanol or acetonitrile.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	+4°C
HANDLING:	After reconstitution, prepare aliquots and store at -20°C. Packaged under inert gas. Protect from light.

Product Description

Potent inhibitor of mammalian HDAC (IC₅₀=15.7nM). Acts as a ligand for the enzyme active site metal ion. Upregulates plasminogen activator inhibitor type 2 (PAI-2) expression with concomitant inhibition of urokinase (u-PA) gene and protein expression in HT-1080 and U-937 cells. Elevates the expression of extracellular matrix proteins fibronectin and gelsolin. Induces apoptosis in P-glyoprotein (Pgp) positive and Pgp negative multidrug resistant cells.

Product Specific Literature References

Oxamflatin: a novel compound which reverses malignant phenotype to normal one via induction of JunD: H. Sonoda, et al.; Oncogene 13, 143 (1996) Abstract
Oxamflatin is a novel antitumor compound that inhibits mammalian histone deacetylase: Y.B. Kim, et al.; Oncogene 18, 2461 (1999) Abstract
The novel anti-tumour agent oxamflatin differentially regulates urokinase and plasminogen activator inhibitor type 2 expression and inhibits urokinase-mediated proteolytic activity: A.E. Dear & R.L. Medcalf; Biochim. Biophys. Acta 1492, 15 (2000) Abstract
Novel mechanisms of apoptosis induced by histone deacetylase inhibitors: M.J. Peart, et al.; Cancer Res. 63, 4460 (2003) Abstract

Further Categories Containing This Product:

HDAC Inhibitors • Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (DNA Interaction & Gene Regulation)

ALX-430-146

Revised 30-Nov-06

PAC-1
SYNONYMS	4-(Phenylmethyl)[[2-hydroxy-3-(2-propenyl)phenyl]methylene]hydrazide-1-piperazine acetic acid
PRODUCT LINE	Cancer
PRODUCT CATEGORY	Antitumor Agents (Apoptosis Inducers)

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-430-146-M010		10 mg	45.00 USD
ALX-430-146-M050		50 mg	180.00 USD

Product Specification

FORMULA:	C₂₃H₂₈N₄O₂
MW:	392.5
CAS NUMBER:	315183-21-2
PURITY:	≥98% (HPLC)
APPEARANCE:	White to off-white solid.
SOLUBILITY:	Soluble in acetonitrile, DMSO, dioxane or methanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

First molecule to directly activate procaspase-3 to caspase-3 in vitro. Has been shown to induce apoptosis in cancer cells.

Product Specific Literature References

Small-molecule activation of procaspase-3 to caspase-3 as a personalized anticancer strategy: K.S. Putt, et al.; Nat. Chem. Biol. 2, 543 (2006) Abstract

Further Categories Containing This Product:

Caspases Other Products

ALX-270-310

Revised 10-Jul-08

PRIMA-1
SYNONYMS	2,2-bis(Hydroxymethyl)-3-quinuclidinone
PRODUCT LINE	Cell Cycle
PRODUCT CATEGORY	p53 Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-310-M001		1 mg	23.00 USD
ALX-270-310-M005		5 mg	101.00 USD

Product Specification

FORMULA:	C₉H₁₅NO₃
MW:	185.2
CAS NUMBER:	5608-24-2
PURITY:	≥95%
APPEARANCE:	White to off-white crystalline solid.
SOLUBILITY:	25mg/ml soluble in 100% ethanol, DMSO or dimethyl formamide; 2.5mg/ml soluble in PBS, pH 7.2 .
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stable for at least 1 year after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.

Product Description

Restores sequence-specific DNA binding and the active conformation to mutant p53 proteins in vitro and in vivo, thus triggering apoptosis of cancer cells.

Product Specific Literature References

Restoration of the tumor suppressor function to mutant p53 by a low-molecular-weight compound: V.J. Bykov, et al.; Nat. Med. 8, 282 (2002) Abstract

Further Categories Containing This Product:

Antitumor Agents (Apoptosis Inducers)

ALX-430-151

Revised 22-Jul-08

RITA
SYNONYMS	Reactivation of p53 and Induction of Tumor Cell Apoptosis 2,5-bis(5-Hydroxymethyl-2-thienyl)furan NSC652287
PRODUCT LINE	Cell Cycle
PRODUCT CATEGORY	p53 Other Products

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-430-151-M001		1 mg	75.00 USD
ALX-430-151-M005		5 mg	290.00 USD

Product Specification

FORMULA:	C₁₄H₁₂O₃S₂
MW:	292.4
CAS NUMBER:	213261-59-7
PURITY:	≥98%
APPEARANCE:	White to yellow crystalline solid.
SOLUBILITY:	Soluble in 100% ethanol (1mg/ml), DMSO (20mg/ml), dimethyl formamide (30mg/ml); 0.5mg/ml soluble in a 1:1 solution of dimethyl formamide: PBS (pH 7.2) (dilute the dimethyl formamide solution with PBS).
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stable for at least two years after receipt when stored at -20°C. We do not recommend storing aqueous solutions for more than one day.

Product Description

Inhibitor of p53/HDM2 interaction. Activator of p53 function in tumors. Potently inhibits the growth of a variety of cancer cell lines in the submicromolar range. It has been suggested that RITA selectively targets cells expressing p53 by other mechanisms than direct binding to the N-terminal domain of p53 [4].

Product Specific Literature References

[1] DNA protein cross-links produced by NSC 652287, a novel thiophene derivative active against human renal cancer cells: W. Nieves-Neira, et al.; Mol. Pharmacol. 56, 478 (1999) Abstract; Full Text
[2] Selective toxicity of the tricyclic thiophene NSC 652287 in renal carcinoma cell lines: differential accumulation and metabolism: M.I. Rivera, et al.; Biochem. Pharmacol. 57, 1283 (1999) Abstract
[3] Small molecule RITA binds to p53, blocks p53-HDM-2 interaction and activates p53 function in tumors: N. Issaeva, et al.; Nat. Med. 10, 1321 (2004) Abstract
[4] NMR indicates that the small molecule RITA does not block p53-MDM2 binding in vitro: M. Krajewski, et al.; Nat. Med. 11, 1135 (2005) Abstract

Further Categories Containing This Product:

Antitumor Agents (Apoptosis Inducers)

ALX-270-377

Revised 07-Feb-05

SC-236
SYNONYMS	4-[5-(4-Chlorophenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamide
PRODUCT LINE	Inflammation
PRODUCT CATEGORY	COX Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-377-M005		5 mg	70.00 USD
ALX-270-377-M025		25 mg	280.00 USD

Product Specification

FORMULA:	C₁₆H₁₁ClF₃N₃O₂S
MW:	401.8
PURITY:	≥95%
APPEARANCE:	White to off-white crystalline powder.
SOLUBILITY:	Soluble in DMSO.
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	-20°C
USE/STABILITY:	Stable for at least 2 years after receipt when stored at -20°C. Stock solutions are stable for 3 months when stored at -20°C.
HANDLING:	Protect from light. Packaged under inert gas.

Product Description

Highly selective and potent inhibitor of cyclooxygenase-2 (IC₅₀=10nM for COX-2 versus IC₅₀=17.8µM for COX-1) with antitumor properties. Exhibits longer half-life time and reduced gastric toxicity in fasting rat model. Has antitumor properties and has been shown to induce apoptosis and bFGF and VEGF-driven angiogenesis. Potent antimetastatic activity against both spontaneous metastases arising following primary tumour excision and experimental metastases.

Product Specific Literature References

A single amino acid difference between cyclooxygenase-1 (COX-1) and -2 (COX-2) reverses the selectivity of COX-2 specific inhibitors: J.K. Gierse, et al.; J. Biol. Chem. 271, 15810 (1996) Abstract; Full Text
Synthesis and biological evaluation of the 1,5-diarylpyrazole class of cyclooxygenase-2 inhibitors: identification of 4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benze nesulfonamide (SC-58635, celecoxib): T.D. Penning, et al.; J. Med. Chem. 40, 1347 (1997) Abstract
Prostaglandin E(2) mediates inhibition of insulin secretion by interleukin-1beta: P.O. Tran, et al.; J. Biol. Chem. 274, 31245 (1999) Abstract; Full Text
COX-2 inhibitors. A new class of antiangiogenic agents: J.L. Masferrer, et al.; Ann. NY Acad. Sci. 889, 84 (1999) Abstract
Inhibition of cyclooxygenase-2 decreases DNA synthesis induced by platelet-derived growth factor in Swiss 3T3 fibroblasts: E. Castano, et al.; J. Pharmacol. Exp. Ther. 293, 509 (2000) Abstract; Full Text
Enhancement of intrinsic tumor cell radiosensitivity induced by a selective cyclooxygenase-2 inhibitor: C. Petersen, et al.; Clin. Cancer Res. 6, 2513 (2000) Abstract; Full Text
Cyclooxygenase-2-derived prostaglandin E2 and lipoxin A4 accelerate resolution of allergic edema in Angiostrongylus costaricensis-infected rats: relationship with concurrent eosinophilia: C. Bandeira-Melo, et al.; J. Immunol. 164, 1029 (2000) Abstract; Full Text
Cyclooxygenase-2 inhibitor SC-236 attenuates mechanical allodynia following nerve root injury in rats: T.A. Deleo, et al.; J. Orthop. Res. 18, 977 (2000) Abstract
Prostaglandins are required for CREB activation and cellular proliferation during liver regeneration: D.A. Rudnick, et al.; PNAS 98, 8885 (2001) Abstract; Full Text
Protective role of cyclooxygenase inhibitors in the adverse action of passive cigarette smoking on the initiation of experimental colitis in rats: X. Guo, et al.; Eur. J. Pharmacol. 411, 193 (2001) Abstract
Neuroprotection by the selective cyclooxygenase-2 inhibitor SC-236 results in improvements in behavioral deficits induced by reversible spinal cord ischemia: P.A. Lapchak, et al.; Stroke 32, 1220 (2001) Abstract; Full Text
Novel target for induction of apoptosis by cyclo-oxygenase-2 inhibitor SC-236 through a protein kinase C-beta(1)-dependent pathway: X.H. Jiang, et al.; Oncogene 21, 6113 (2002) Abstract
Cyclooxygenase-2 inhibitor (SC-236) suppresses activator protein-1 through c-Jun NH2-terminal kinase: B.C. Wong, et al.; Gastroenterology 126, 136 (2004) Abstract

Further Categories Containing This Product:

Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (Apoptosis Inducers)

ALX-270-400

Revised 31-Mar-05

SU 9516
SYNONYMS	3-[1-(3H-Imidazol-4-yl)-meth-(Z)-ylidene]-5-methoxy-1,3-dihydro-indol-2-one
PRODUCT LINE	Cell Cycle
PRODUCT CATEGORY	CDK & Cyclin Inhibitors

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-270-400-M005		5 mg	80.00 USD
ALX-270-400-M025		25 mg	320.00 USD

Product Specification

FORMULA:	C₁₃H₁₁N₃O₂
MW:	241.3
PURITY:	≥95%
APPEARANCE:	Yellow to orange solid.
SOLUBILITY:	Soluble in DMSO (10mg/ml).
SHIPPING:	SHIPPED ON BLUE ICE
LONG TERM STORAGE:	+4°C
HANDLING:	Protect from light. Packaged under inert gas.

Product Description

Cell permeable, potent, selective and ATP-competitive inhibitor of CDK2/cyclin A (IC₅₀=22nM), CDK1/cyclin B (IC₅₀=40nM) and CDK4/cyclin D1 (IC₅₀=200nM). Has no effect on the activity of PKC, p38, PDGFRβ and EGFR (IC₅₀>10µM). Displays anti-proliferative and pro-apoptotic properties in tumor cells. Inhibits proliferation of growth factor-stimulated colon carcinoma cells by binding to CDK2 and thus preventing the phosphorylation of pRb and its dissociation from E2F.

Product Specific Literature References

A novel cdk2-selective inhibitor, SU9516, induces apoptosis in colon carcinoma cells: M.E. Lane, et al.; Cancer Res. 61, 6170 (2001) Abstract
SU9516, a cyclin-dependent kinase 2 inhibitor, promotes accumulation of high molecular weight E2F complexes in human colon carcinoma cells: B. Yu, et al.; Biochem Pharmacol. 64, 1091 (2002) Abstract
SU9516: biochemical analysis of cdk inhibition and crystal structure in complex with cdk2: D.J. Moshinsky, et al.; BBRC 310, 1026 (2003) Abstract
Novel pyrrolyllactone and pyrrolyllactam indolinones as potent cyclin-dependent kinase 2 inhibitors: X. Li, et al.; Bioorg. Med. Chem. Lett. 13, 1939 (2003) Abstract

Further Categories Containing This Product:

Antitumor Agents (Anti-proliferative) • Antitumor Agents (Enzyme Inhibitors) • Antitumor Agents (Apoptosis Inducers)

ALX-400-053

Revised 21-Apr-08

Teniposide
SYNONYMS	(5R,5aR,8aR,9S)-5,8,8a,9-Tetrahydro-5-(4-hydroxy-3,5-dimethoxyphenyl)-9-[[4,6-O-[(R)-2-thienylmethylene]-β-D-glucopyranosyl]oxy]furo[3’,4’:6,7]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one 4’-Demethylepipodophyllotoxin-β-D-thenylidine glucoside
PRODUCT LINE	Cancer
PRODUCT CATEGORY	Antitumor Agents (DNA Interaction & Gene Regulation)

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-400-053-M025		25 mg	55.00 USD
ALX-400-053-M100		100 mg	165.00 USD

Product Specification

FORMULA:	C₃₂H₃₂O₁₃S
MW:	656.7
CAS NUMBER:	29767-20-2
MERCK INDEX:	14: 9145
SOURCE/HOST:	Semisynthetic derivative of podophyllotoxin.
PURITY:	≥97% (HPLC)
APPEARANCE:	White to off-white powder.
SOLUBILITY:	Soluble in acetone or dimethyl formamide; slightly soluble in methanol; insoluble in water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	TOXIC. MAY BE CARCINOGENIC.

Product Description

Glycoside-derivative of podophyllotoxin. Has cytostatic effect. Inhibits topoisomerase II. Induces apoptosis.

Product Specific Literature References

Role of topoisomerase II in mediating epipodophyllotoxin-induced DNA cleavage: W. Ross, et al.; Cancer Res. 44, 5857 (1984) Abstract; Full Text
Human cytochrome P450 metabolism of teniposide and etoposide: M.V. Relling, et al.; J. Pharmacol. Exp. Ther. 261, 491 (1992) Abstract
Topoisomerase II as a target of VM-26 and 4’-(9-acridinylamino)methanesulfon-m-aniside in atypical multidrug resistant human small cell lung carcinoma cells: S de Jong, et al.; Cancer Res. 53, 1064 (1993) Abstract; Full Text
Topoisomerase II trapping agent teniposide induces apoptosis and G2/M or S phase arrest of oral squamous cell carcinoma: J. Li, et al.; World J. Surg. Oncol. 4, 41 (2006) Abstract; Full Text

Related Products

ALX-630-086

Podophyllotoxin

Further Categories Containing This Product:

Antitumor Agents (Apoptosis Inducers) • Natural Products - Antitumor Reagents • Topoisomerase Inhibitors Other Products • Antitumor Agents (Enzyme Inhibitors)

ALX-350-259

Revised 17-Dec-07

Triptolide
SYNONYMS	PG490
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products - Immunomodulators

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-259-M001		1 mg	70.00 USD
ALX-350-259-M005		5 mg	280.00 USD

Product Specification

FORMULA:	C₂₀H₂₄O₆
MW:	360.4
CAS NUMBER:	38748-32-2
SOURCE/HOST:	Isolated from Tripterygium wilfordii.
PURITY:	≥98%
APPEARANCE:	White solid.
SOLUBILITY:	Soluble in DMSO or 100% ethanol.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C

Product Description

Immunosuppressive agent with anti-inflammatory and antitumor properties. More effective in preventing T cell proliferation and interferon-γ production than FK506 (Prod. No. ALX-380-008). Induces apoptosis in T cells by activating DEVD cleaving caspases. Blocks TNF-α mediated induction of c-IAP1 and c-IAP2 and NF-κB activation.

Product Specific Literature References

Triptolide induces apoptotic death of T lymphocyte: Y. Yang, et al.; Immunopharmacology 40, 139 (1998) Abstract
Triptolide is more effective in preventing T cell proliferation and interferon-gamma production than is FK506: M.A. Chan, et al.; Phytother. Res. 13, 464 (1999) Abstract
Immunosuppressant PG490 (triptolide) inhibits T-cell interleukin-2 expression at the level of purine-box/nuclear factor of activated T- cells and NF-kappaB transcriptional activation: D. Qiu, et al.; J. Biol. Chem. 274, 13443 (1999) Abstract; Full Text
PG490 (triptolide) cooperates with tumor necrosis factor-alpha to induce apoptosis in tumor cells: K.Y. Lee, et al.; J. Biol. Chem. 274, 13451 (1999) Abstract; Full Text
Immunosuppressive and anti-inflammatory mechanisms of triptolide, the principal active diterpenoid from the Chinese medicinal herb Tripterygium wilfordii Hook. f:: D. Qiu & P.N. Kao; Drugs R. D. 4, 1 (2003), (Review) Abstract
Triptolide, a diterpenoid triepoxide, induces antitumor proliferation via activation of c-Jun NH2-terminal kinase 1 by decreasing phosphatidylinositol 3-kinase activity in human tumor cells: Y. Miyata, et al.; BBRC 336, 1081 (2005) Abstract
Triptolide, an inhibitor of the human heat shock response that enhances stress-induced cell death: S.D. Westerheide, et al.; J. Biol. Chem. 281, 9616 (2006) Abstract
Triptolide induces caspase-dependent cell death mediated via the mitochondrial pathway in leukemic cells: B.Z. Carter, et al.; Blood 108, 630 (2006) Abstract

Further Categories Containing This Product:

Natural Products - NF-kB Pathway Inhibitors • Natural Products - Anti-inflammatory Agents • Antitumor Agents (Apoptosis Inducers) • Natural Products - Apoptosis Inducers & Inhibitors • NF-kB Pathway Inhibitors • Natural Products - Antitumor Reagents

ALX-350-257

Revised 08-Oct-08

Vinblastine . sulfate
SYNONYMS	Vincaleukoblastine . sulfate
PRODUCT LINE	Natural Products / Antibiotics
PRODUCT CATEGORY	Natural Products for Cell Cycle Research

Ordering Information

Product Numbers:	Format:	Size:	Unit Price:	Quantity:	Add To Cart
ALX-350-257-M005		5 mg	45.00 USD
ALX-350-257-M025		25 mg	190.00 USD

Product Specification

FORMULA:	C₄₆H₅₈N₄O₉ . H₂SO₄
MW:	811.0 . 98.1
CAS NUMBER:	143-67-9
MERCK INDEX:	14: 9982
SOURCE/HOST:	Semisynthetic from catharanthine or vindoline.
PURITY:	≥98%
APPEARANCE:	White powder.
SOLUBILITY:	Soluble in DMSO, methanol or water.
SHIPPING:	AMBIENT
LONG TERM STORAGE:	-20°C
HAZARD:	TOXIC. MAY BE CARCINOGENIC.

Product Description

Plant alkaloid that arrests the cell cycle in G2/M phase by blocking mitotic spindle formation. Depolymerizes microtubul