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GDC-0941

Item № 11600
CAS № 957054-30-7
Purity ≥98%
product image
                (CAS 957054-30-7)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     10 mg $119.00 0.00
     50 mg $298.00 0.00
     100 mg $476.00 0.00

Pricing updated 2019-07-18. Prices are subject to change without notice.

Description
Synonyms
  • GNE-0941
  • Pictilisib
  • Pictrelisib

The phosphatidylinositol 3-kinase (PI3K) signaling pathway has central roles in cell growth, development, and survival.1,2 GDC-0941 is a potent pan inhibitor of class I catalytic subunits of PI3K, inhibiting p110α, β, δ, and γ with IC50 values of 3, 33, 3, and 75 nM, respectively.3,4 It is much less effective against class II-IV isoforms of PI3K and against mTOR.3,5 GDC-0941 inhibits the growth of certain types of cancer cells and blocks signaling through PI3K to Akt, both in cells and in vivo.3,6

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Technical Information
Formal Name
2-(1H-indazol-4-yl)-6-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-4-(4-morpholinyl)-thieno[3,2-d]pyrimidine
CAS Number
957054-30-7
Synonyms
  • GNE-0941
  • Pictilisib
  • Pictrelisib
Molecular Formula
C23H27N7O3S2
Formula Weight
513.6
Purity
≥98%
Formulation
A crystalline solid
λmax
213, 260, 319 nm
SMILES
CS(N(CC1)CCN1CC(S2)=CC3=C2C(N4CCOCC4)=NC(C5=C(C=NN6)C6=CC=C5)=N3)(=O)=O
InChI Code
InChI=1S/C23H27N7O3S2/c1-35(31,32)30-7-5-28(6-8-30)15-16-13-20-21(34-16)23(29-9-11-33-12-10-29)26-22(25-20)17-3-2-4-19-18(17)14-24-27-19/h2-4,13-14H,5-12,15H2,1H3,(H,24,27)
InChI Key
LHNIIDJUOCFXAP-UHFFFAOYSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
Downloads & Resources
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Additional Information

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References & Product Citations
Product Description References

1. Hennessy, B.T., Smith, D.L., Ram, P.T., et al. Exploiting the PI3K/AKT pathway for cancer drug discovery Nature Reviews.Drug Discovery 4, 988-1004 (2005).

2. Hirsch, E., Ciraolo, E., Ghigo, A., et al. Taming the PI3K team to hold inflammation and cancer at bay Pharmacology & Therapeutics 118, 192-205 (2008).

3. Folkes, A.J., Ahmadi, K., Alderton, W.K., et al. The identification of 2-(1H-indazol-4-yl)-6-(4-methanesulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2-d]pyrimidine (GDC-0941) as a potent, selective, orally bioavailable inhibitor of class I PI3 kinase for the treatment of cancer Journal of Medicinal Chemistry 51(18), 5522-5532 (2008).

4. Berndt, A., Miller, S., Williams, O., et al. The p110δ structure: Mechanisms for selectivity and potency of new PI(3)K inhibitors Nature Chemical Biology 6(2), 117-124 (2010).

5. Sutherlin, D.P., Sampath, D., Berry, M., et al. Discovery of (thienopyrimidin-2-yl)aminopyrimidines as potent, selective, and orally available pan-PI3-kinase and dual pan-PI3-kinase/mTOR inhibitors Journal of Medicinal Chemistry 53(3), 1086-1097 (2010).

6. Raynaud, F.I., Eccles, S.A., Patel, S., et al. Biological properties of potent inhibitors of class I phosphatidylinositide 3-kinases: From PI-103 through PI-540, PI-620 to the oral agent GDC-0941 Molecular Cancer Therapeutics 8(7), 1725-1738 (2009).

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