An ALK2R206H inhibitor
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BLU-782

Item No. 35490

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[6-[5-[4-ethoxy-1-(1-methylethyl)-4-piperidinyl]-2-pyridinyl]pyrrolo[1,2-b]pyridazin-4-yl]-1-piperazinecarboxylic acid, (3R)-tetrahydro-3-furanyl ester
CAS Number
2141955-96-4
Synonyms
  • Activin Receptor-like Kinase 2 Inhibitor 1
  • ALK2-IN-1
  • Fidrisertib
Molecular Formula
C31H42N6O4
Formula Weight
562.7
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 1 mg/ml
λmax
255, 320 nm
SMILES
CCOC1(C2=CN=C(C3=CN(N=CC=C4N5CCN(CC5)C(O[C@@H]6CCOC6)=O)C4=C3)C=C2)CCN(CC1)C(C)C
InChi Code
InChI=1S/C31H42N6O4/c1-4-40-31(9-12-34(13-10-31)23(2)3)25-5-6-27(32-20-25)24-19-29-28(7-11-33-37(29)21-24)35-14-16-36(17-15-35)30(38)41-26-8-18-39-22-26/h5-7,11,19-21,23,26H,4,8-10,12-18,22H2,1-3H3/t26-/m1/s1
InChi Key
SWVYYNLRVIYURK-AREMUKBSSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $62

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    5 mg

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    10 mg

    $395

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    25 mg

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    Product Description

    BLU-782 is an inhibitor of activin receptor-like kinase 2 (ALK2) containing an arginine-to-histidine substitution mutation at position 206 (ALK2R206H), an activating mutation found in patients with fibrodysplasia ossificans progressiva (FOP), which is characterized by progressive heterotopic ossification, or diffuse intrinsic pontine glioma (DIPG), which is a type of pediatric brain stem cancer.1 It binds to ALK2R206H (IC50 = ≤10 nM) and reduces phosphorylation of the ALK2 substrate SMAD1 at serine 463 (Ser463) and Ser465 in HEK293 cells expressing ALK2R206H (IC50 = ≤100 nM).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Fleming, P.E., Hodous, B.L., Kim, J.L., et al. Inhibitors of activin receptor-like kinase. (2017).