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MedKoo product information:
Saridegib
Description of Saridegib (IPI-926):
Saridegib (IPI-926) is an orally bioavailable, cyclopamine-derived (for
structure comparison see Fig 1) inhibitor of
the Hedgehog (Hh) pathway with potential antineoplastic activity.
Specifically, Hedgehog pathway inhibitor IPI-926 binds to and
inhibits the cell membrane-spanning G-protein coupled receptor SMO,
which may result in the suppression of Hh pathway signaling and a
decrease in tumor cell proliferation and survival. SMO is activated
upon binding of Hh ligand to the cell surface receptor Patched
(PTCH); inappropriate activation of Hh signaling and uncontrolled
cellular proliferation may be associated with SMO mutations. The Hh
signaling pathway plays an important role in proliferation of
neuronal precursor cells in the developing cerebellum and other
tissues. Check for
active clinical trials or
closed clinical trials using this agent. (NCI
Thesaurus).
Current developer:
Infinity Pharmaceuticals, Inc.
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MedKoo Code#: 201572
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Name:
Saridegib
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CAS#: 1037210-93-7
Synonym: IPI 926.
Saridegib
IUPAC/Chemical name:
N-((2S,3R,3aS,3'R,4a'R,6S,6a'R,6b'S,7aR,12a'S,12b'S)-3,6,11',12b'-tetramethyl-2',3a,3',4,4',4a',5,5',6,6',6a',6b',7,7a,7',8',10',12',12a',12b'-icosahydro-1'H,3H-spiro[furo[3,2-b]pyridine-2,9'-naphtho[2,1-a]azulen]-3'-yl)methanesulfonamide
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Chemical structure:
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Theoretical analysis
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Chemical Formula: C29H48N2O3S
Exact Mass: 504.33856
Molecular Weight: 504.76802
Elemental Analysis: C, 69.00; H, 9.58; N,
5.55; O, 9.51; S, 6.35
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Availability and price:
This agent is not in
stock, and is available through custom synthesis.
To inquire the quotation and lead time of custom synthesis for this agent, please send email to
sales@medkoo.com to describe your needs. A representative
will respond your email shortly. We offer big discount for orders of bulk quantities.
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Quality control
data:
Product will be shipped with
supporting analytical data.
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Information about this agent
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Fig 1.
Chemical structure comparison between IPI-926 and cyclopamine
IPI-926
is currently developed by Infinity Pharmaceuticals, Inc. Malignant
activation of the Hedgehog pathway is implicated in multiple cancer
settings and Infinity's development strategy is designed to enable
IPI-926 to target a broad range of critical oncology targets - from the
tumor cell to the cancer microenvironment. This broadly applicable,
targeted approach represents an innovative method for fighting cancer
and has potential in treating a range of cancers, including pancreatic
cancer, small cell lung cancer, ovarian cancer, bladder cancer,
medulloblastoma, basal cell carcinoma, and certain hematological
malignancies.
1. Austad, B.; Bahadoor, A.; Belani, J.
D.; Janardanannair, S.; Johannes, C. W.; Keaney, G. F.; Lo, C. K.;
Wallerstein, S. L. Enzymatic transamination of cyclopamine analogs.
WO2011017551A1.
2. Austad, B.; Behnke, M. L.; Castro, A. C.; Grogan, M. J.;
Janardanannair, S.; Lescarbeau, A.; Peluso, S.; Tremblay, M. Preparation
of cyclopamine analogs which inhibit the hedgehog pathway for
therapeutic use as anticancer agents. US7812164B2.
3. Austad, B.; Janardanannair, S.; Lescarbeau, A.; Tremblay, M.
Preparation of cyclopamine analogs for therapeutic use in anticancer
pharmaceutical compositions which inhibit the hedgehog pathway.
WO2008083248A2, 2008.
4. Austad, B.; Janardanannair, S.; Lescarbeau, A.; Tremblay, M.; Grayzel,
D.; Matsui, W. Preparation of cyclopamine analogs for therapeutic use in
anticancer pharmaceutical compositions which inhibit the hedgehog
pathway. WO2008083252A2, 2008.
5. Austad, B. C. Methods for stereoselective reduction. WO2009086451A1,
2009.
6. Carter, B.; Lee, J. J.; Sheikh, H. Oral formulations of IPI-926.
WO2011057222A1.
7. Gould, A.; Missailidis, S., Targeting the Hedgehog pathway: the
development of cyclopamine and the development of anti-cancer drugs
targeting the Hedgehog pathway. Mini-Rev. Med. Chem. 11, (3), 200-213.
8. Grayzel, D.; Ross, R.; MacDougall, J. Cancer treatments using
hedgehog inhibitors and chemotherapy. WO2009086416A1, 2009.
9. Kottmann, A. H. Shh signaling regulation and methods thereof for
upregulating GDNF and treating neurodegenerative disorder.
WO2010117800A2.
10. Lin, T. L.; Wang, Q. H.; Brown, P.; Peacock, C.; Merchant, A. A.;
Brennan, S.; Jones, E.; McGovern, K.; Neil, W. D.; Sakamoto, K. M.;
Matsui, W., Self-renewal of acute lymphocytic leukemia cells is limited
by the Hedgehog pathway inhibitors cyclopamine and IPI-926. PLoS One 5,
(12), e15262.
11. MacDougall, J.; West, K. A. Therapeutic cancer treatments using
hedgehog inhibitors combined with EGFR-tyrosine kinase inhibitors.
US20100297118A1.
12. McGovern, K. J.; Read, M.; Ross, R. W. Use of hedgehog inhibitor in
combination with other chemotherapeutics in cancer treatment.
US20100222287A1.
13. Olive, K. P.; Jacobetz, M. A.; Davidson, C. J.; Gopinathan, A.;
McIntyre, D.; Honess, D.; Madhu, B.; Goldgraben, M. A.; Caldwell, M. E.;
Allard, D.; Frese, K. K.; DeNicola, G.; Feig, C.; Combs, C.; Winter, S.
P.; Ireland-Zecchini, H.; Reichelt, S.; Howat, W. J.; Chang, A.; Dhara,
M.; Wang, L.; Rueckert, F.; Gruetzmann, R.; Pilarsky, C.; Izeradjene,
K.; Hingorani, S. R.; Huang, P.; Davies, S. E.; Plunkett, W.; Egorin,
M.; Hruban, R. H.; Whitebread, N.; McGovern, K.; Adams, J.; Iacobuzio-Donahue,
C.; Griffiths, J.; Tuveson, D. A., Inhibition of Hedgehog Signaling
Enhances Delivery of Chemotherapy in a Mouse Model of Pancreatic Cancer.
Science (Washington, DC, U. S.) 2009, 324, (5933), 1457-1461.
14. Olive, K. P.; Tuveson, D. Hedgehog pathway inhibitors.
WO2010085654A1.
15. Tao, C.; Desai, N. P.; Soon-Shiong, P. Combination therapy with
nanoparticle compositions of taxane and hedgehog inhibitors for treating
proliferative disease such as cancer. WO2011025838A1.
16. Travaglione, V.; Macdougall, J.; McGovern, K. J. Methods and
compositions for treating hedgehog-associated cancers. WO2011063309A1.
17. Tremblay, M. R.; Lescarbeau, A.; Grogan, M. J.; Tan, E.; Lin, G.;
Austad, B. C.; Yu, L.-C.; Behnke, M. L.; Nair, S. J.; Hagel, M.; White,
K.; Conley, J.; Manna, J. D.; Alvarez-Diez, T. M.; Hoyt, J.; Woodward,
C. N.; Sydor, J. R.; Pink, M.; MacDougall, J.; Campbell, M. J.; Cushing,
J.; Ferguson, J.; Curtis, M. S.; McGovern, K.; Read, M. A.; Palombella,
V. J.; Adams, J.; Castro, A. C., Discovery of a Potent and Orally Active
Hedgehog Pathway Antagonist (IPI-926). J. Med. Chem. 2009, 52, (14),
4400-4418.
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